Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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1323 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
1323 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 55 Human Functional pEC50 = 10.2 10.2 -58 8
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
1324 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16154396 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727.0 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
44285019 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
57514683 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
91898441 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
DB04931 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
CHEMBL413212 213055 None 0 Human Functional pEC50 = 10.2 10.2 -3 4
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
1324 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
1324 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16154396 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16154396 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16197727 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16197727.0 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727.0 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
44285019 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
44285019 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
57514683 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
57514683 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
91898441 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
91898441 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
DB04931 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
DB04931 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
1324 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
16154396 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727.0 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
44285019 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
57514683 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
91898441 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
DB04931 302 None 25 Mouse Functional pEC50 = 10.2 10.2 -6 9
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0490843
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01417
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R by alphascreen cAMP assayAgonist activity at mouse MC3R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
1324 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16154396 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727.0 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
44285019 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
57514683 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
91898441 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
DB04931 302 None 25 Mouse Functional pEC50 = 10.1 10.1 -6 9
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
1324 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
16154396 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
16197727 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
16197727.0 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
44285019 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
57514683 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
91898441 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
DB04931 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
1324 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727.0 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 302 None 25 Mouse Functional pEC50 = 10.0 10.0 -6 9
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
1324 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727.0 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 302 None 25 Mouse Functional pEC50 = 10 10.0 -6 9
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
1324 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16154396 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16197727 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16197727.0 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
44285019 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
57514683 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
91898441 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
CHEMBL441738 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
DB04931 302 None 25 Rat Functional pEC50 = 10 10.0 -1 9
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
168284256 190946 None 0 Human Functional pEC50 = 10.0 10.0 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 190946 None 0 Human Functional pEC50 = 10.0 10.0 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168281421 190957 None 0 Human Functional pEC50 = 10.0 10.0 10 3
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 190957 None 0 Human Functional pEC50 = 10.0 10.0 10 3
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL429236 213516 None 0 Mouse Functional pEC50 = 10.0 10.0 -5 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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/jm010061n
1324 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727.0 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 302 None 25 Human Functional pEC50 = 9.9 9.9 -15 9
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
1324 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16154396 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16197727 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16197727.0 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
44285019 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
57514683 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
91898441 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
DB04931 302 None 25 Mouse Functional pEC50 = 9.9 9.9 -6 9
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
127036484 136445 None 0 Mouse Functional pEC50 = 9.8 9.8 -3 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(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](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136445 None 0 Mouse Functional pEC50 = 9.8 9.8 -3 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(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](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
11993702 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 18 Human Functional pEC50 = 9.8 9.8 1 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
168271934 190085 None 0 Human Functional pEC50 = 9.8 9.8 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 190085 None 0 Human Functional pEC50 = 9.8 9.8 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
1323 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
92432 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL430239 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None None 10.1021/jm010524p
44310104 81588 None 0 Mouse Functional pEC50 = 9.8 9.8 -7 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)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)NC1=O 10.1021/jm0303608
CHEMBL216295 81588 None 0 Mouse Functional pEC50 = 9.8 9.8 -7 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)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)NC1=O 10.1021/jm0303608
CHEMBL386081 212375 None 0 Mouse Functional pEC50 = 9.8 9.8 -8 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010061n
1323 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
92432 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL430239 2688 None 55 Mouse Functional pEC50 = 9.8 9.8 -5 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
1323 2688 None 55 Mouse Functional pEC50 = 9.7 9.7 -5 8
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
92432 2688 None 55 Mouse Functional pEC50 = 9.7 9.7 -5 8
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
CHEMBL430239 2688 None 55 Mouse Functional pEC50 = 9.7 9.7 -5 8
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
127036484 136445 None 0 Mouse Functional pEC50 = 9.7 9.7 -3 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(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](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136445 None 0 Mouse Functional pEC50 = 9.7 9.7 -3 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(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](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
168289404 191312 None 0 Human Functional pEC50 = 9.7 9.7 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 191312 None 0 Human Functional pEC50 = 9.7 9.7 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16154396 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16197727 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16197727.0 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
44285019 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
57514683 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
91898441 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
DB04931 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
1324 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16154396 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16197727 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16197727.0 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
44285019 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
57514683 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
91898441 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
DB04931 302 None 25 Mouse Functional pEC50 = 9.7 9.7 -6 9
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 assayAgonist 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
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
CHEMBL428615 213460 None 0 Human Functional pEC50 = 9.7 9.7 -10 5
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
118722938 116239 None 0 Mouse Functional pEC50 = 9.7 9.7 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358546 116239 None 0 Mouse Functional pEC50 = 9.7 9.7 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722941 116242 None 0 Mouse Functional pEC50 = 9.7 9.7 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358549 116242 None 0 Mouse Functional pEC50 = 9.7 9.7 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1323 2688 None 55 Human Functional pEC50 = 9.7 9.7 -58 8
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 55 Human Functional pEC50 = 9.7 9.7 -58 8
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 55 Human Functional pEC50 = 9.7 9.7 -58 8
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
118722937 116238 None 0 Mouse Functional pEC50 = 9.7 9.7 -5 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358545 116238 None 0 Mouse Functional pEC50 = 9.7 9.7 -5 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL2371851 210139 None 0 Mouse Functional pEC50 = 9.7 9.7 -5 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None 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/jm0490843
122194229 123983 None 0 Mouse Functional pEC50 = 9.7 9.7 -8 5
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(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 10.1016/j.bmcl.2015.09.046
CHEMBL3629347 123983 None 0 Mouse Functional pEC50 = 9.7 9.7 -8 5
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(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 10.1016/j.bmcl.2015.09.046
16132144 209279 None 36 Mouse Functional pEC50 = 9.7 9.7 -2 8
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 assayAgonist 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
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/acsmedchemlett.9b00198
16133793 209279 None 36 Mouse Functional pEC50 = 9.7 9.7 -2 8
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 assayAgonist 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
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/acsmedchemlett.9b00198
44273719 209279 None 36 Mouse Functional pEC50 = 9.7 9.7 -2 8
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 assayAgonist 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
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/acsmedchemlett.9b00198
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.7 9.7 -2 8
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 assayAgonist 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
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/acsmedchemlett.9b00198
168284733 191624 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 191624 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
122194229 123983 None 0 Mouse Functional pEC50 = 9.6 9.6 -8 5
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(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 10.1016/j.bmcl.2015.10.095
CHEMBL3629347 123983 None 0 Mouse Functional pEC50 = 9.6 9.6 -8 5
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(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 10.1016/j.bmcl.2015.10.095
1324 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16154396 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16197727 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16197727.0 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
44285019 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
57514683 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
91898441 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
DB04931 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
CHEMBL405087 212541 None 0 Rat Functional pEC50 = 9.6 9.6 -2 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL414965 213166 None 0 Rat Functional pEC50 = 9.6 9.6 -4 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1324 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16154396 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727.0 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
44285019 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
57514683 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
91898441 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
DB04931 302 None 25 Mouse Functional pEC50 = 9.6 9.6 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
1324 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 25 Human Functional pEC50 = 9.6 9.6 -15 9
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
1323 2688 None 55 Human Functional pEC50 = 9.6 9.6 -58 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 55 Human Functional pEC50 = 9.6 9.6 -58 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 55 Human Functional pEC50 = 9.6 9.6 -58 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL267794 210733 None 0 Mouse Functional pEC50 = 9.6 9.6 -7 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
168272660 190433 None 0 Human Functional pEC50 = 9.6 9.6 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 190433 None 0 Human Functional pEC50 = 9.6 9.6 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
118722936 116237 None 0 Mouse Functional pEC50 = 9.5 9.5 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358544 116237 None 0 Mouse Functional pEC50 = 9.5 9.5 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722944 116245 None 0 Mouse Functional pEC50 = 9.5 9.5 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358552 116245 None 0 Mouse Functional pEC50 = 9.5 9.5 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL410763 212838 None 0 Mouse Functional pEC50 = 9.5 9.5 -7 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
1324 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 25 Human Functional pEC50 = 9.5 9.5 -15 9
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
168270124 189955 None 0 Human Functional pEC50 = 9.5 9.5 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 189955 None 0 Human Functional pEC50 = 9.5 9.5 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168276507 190265 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 190265 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
1324 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
16154396 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
16197727 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
16197727.0 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
44285019 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
57514683 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
91898441 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
DB04931 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm800291b
1324 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16154396 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16197727 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16197727.0 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
44285019 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
57514683 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
91898441 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
DB04931 302 None 25 Mouse Functional pEC50 = 9.5 9.5 -6 9
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16157270 212553 None 14 Human Functional pEC50 = 9.5 9.5 22 7
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 212553 None 14 Human Functional pEC50 = 9.5 9.5 22 7
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
16157270 212553 None 14 Human Functional pEC50 = 9.5 9.5 22 7
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 212553 None 14 Human Functional pEC50 = 9.5 9.5 22 7
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
168293710 192166 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 192166 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289457 191380 None 0 Human Functional pEC50 = 9.5 9.5 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 191380 None 0 Human Functional pEC50 = 9.5 9.5 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
16154396 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
16197727 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
16197727.0 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
44285019 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
57514683 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
91898441 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
DB04931 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02041
CHEMBL413912 213100 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC[C@H](C)[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](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 10.1016/j.bmcl.2004.07.046
1324 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16154396 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727.0 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
44285019 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
57514683 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
91898441 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
DB04931 302 None 25 Human Functional pEC50 = 9.4 9.4 -15 9
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL264536 210627 None 5 Mouse Functional pEC50 = 9.4 9.4 -8 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm010061n
168281389 190922 None 0 Human Functional pEC50 = 9.4 9.4 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=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]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 190922 None 0 Human Functional pEC50 = 9.4 9.4 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=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]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
44415913 79951 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 79951 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
16132144 209279 None 36 Mouse Functional pEC50 = 9.4 9.4 -2 8
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
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/acsmedchemlett.5b00053
16133793 209279 None 36 Mouse Functional pEC50 = 9.4 9.4 -2 8
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
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/acsmedchemlett.5b00053
44273719 209279 None 36 Mouse Functional pEC50 = 9.4 9.4 -2 8
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
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/acsmedchemlett.5b00053
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.4 9.4 -2 8
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
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/acsmedchemlett.5b00053
1324 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16154396 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16197727 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16197727.0 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
44285019 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
57514683 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
91898441 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
DB04931 302 None 25 Mouse Functional pEC50 = 9.4 9.4 -6 9
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
118722933 116235 None 0 Mouse Functional pEC50 = 9.4 9.4 -8 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358541 116235 None 0 Mouse Functional pEC50 = 9.4 9.4 -8 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
44416057 81191 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 81191 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
16132144 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
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 10.1016/j.bmcl.2015.09.046
16133793 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
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 10.1016/j.bmcl.2015.09.046
44273719 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
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 10.1016/j.bmcl.2015.09.046
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
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 10.1016/j.bmcl.2015.09.046
16132144 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
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/jm0492756
16133793 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
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/jm0492756
44273719 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
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/jm0492756
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
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/jm0492756
16132144 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 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/jm0490843
16133793 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 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/jm0490843
44273719 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 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/jm0490843
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.3 9.3 -2 8
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 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/jm0490843
101670969 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
16131138 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
44349184 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
53310908 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
91898438 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL438402 168896 None 23 Mouse Functional pEC50 = 9.3 9.3 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
118722942 116243 None 0 Mouse Functional pEC50 = 9.2 9.2 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358550 116243 None 0 Mouse Functional pEC50 = 9.2 9.2 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
168295726 192405 None 0 Human Functional pEC50 = 9.2 9.2 -6 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 192405 None 0 Human Functional pEC50 = 9.2 9.2 -6 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
118722943 116244 None 0 Mouse Functional pEC50 = 9.2 9.2 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358551 116244 None 0 Mouse Functional pEC50 = 9.2 9.2 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
16132144 209279 None 36 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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/jm00018a005
16133793 209279 None 36 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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/jm00018a005
44273719 209279 None 36 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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/jm00018a005
CHEMBL214332 209279 None 36 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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/jm00018a005
10408 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
10408 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 28 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL408257 212704 None 0 Human Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL None None None CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
168283616 191239 None 0 Human Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 191239 None 0 Human Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
42630327 155871 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)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)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155871 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)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)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
16132144 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 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/jm010061n
16133793 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 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/jm010061n
44273719 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 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/jm010061n
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 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/jm010061n
16132144 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
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/acs.jmedchem.5b01894
16133793 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
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/acs.jmedchem.5b01894
44273719 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
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/acs.jmedchem.5b01894
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
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/acs.jmedchem.5b01894
16132144 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
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/jm010524p
16133793 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
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/jm010524p
44273719 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
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/jm010524p
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
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/jm010524p
16132144 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 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/jm0303608
16133793 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 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/jm0303608
44273719 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 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/jm0303608
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 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/jm0303608
16132144 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
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 10.1016/j.bmcl.2003.08.078
16133793 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
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 10.1016/j.bmcl.2003.08.078
44273719 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
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 10.1016/j.bmcl.2003.08.078
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 9.1 9.1 -2 8
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
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 10.1016/j.bmcl.2003.08.078
1324 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727.0 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1324 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 25 Human Functional pEC50 = 9.1 9.1 -15 9
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
1324 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16154396 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16197727 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16197727.0 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
44285019 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
57514683 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
91898441 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
DB04931 302 None 25 Mouse Functional pEC50 = 9.1 9.1 -6 9
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
118722930 116233 None 0 Mouse Functional pEC50 = 9.1 9.1 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358539 116233 None 0 Mouse Functional pEC50 = 9.1 9.1 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
118722926 116230 None 0 Mouse Functional pEC50 = 9.0 9.0 -7 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=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)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358535 116230 None 0 Mouse Functional pEC50 = 9.0 9.0 -7 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=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)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
168271237 190488 None 0 Human Functional pEC50 = 9.0 9.0 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 190488 None 0 Human Functional pEC50 = 9.0 9.0 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL2369484 209627 None 0 Mouse Functional pEC50 = 9 9.0 -4 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)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](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44415914 139270 None 0 Human Functional pEC50 = 9 9.0 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 139270 None 0 Human Functional pEC50 = 9 9.0 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
145966364 164120 None 0 Human Functional pEC50 = 9 9.0 3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 164120 None 0 Human Functional pEC50 = 9 9.0 3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL2372859 210300 None 1 Mouse Functional pEC50 = 9.0 9.0 -5 3
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm501027w
16132144 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 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 10.1016/j.bmcl.2005.02.068
16133793 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 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 10.1016/j.bmcl.2005.02.068
44273719 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 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 10.1016/j.bmcl.2005.02.068
CHEMBL214332 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 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 10.1016/j.bmcl.2005.02.068
16132144 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
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 10.1016/j.bmcl.2004.10.020
16133793 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
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 10.1016/j.bmcl.2004.10.020
44273719 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
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 10.1016/j.bmcl.2004.10.020
CHEMBL214332 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
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 10.1016/j.bmcl.2004.10.020
16132144 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
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)
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 10.1016/j.bmcl.2005.05.109
16133793 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
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)
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 10.1016/j.bmcl.2005.05.109
44273719 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
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)
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 10.1016/j.bmcl.2005.05.109
CHEMBL214332 209279 None 36 Human Functional pEC50 = 9.0 9.0 -7 8
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)
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 10.1016/j.bmcl.2005.05.109
CHEMBL428801 213472 None 0 Human Functional pEC50 = 9.0 9.0 -26 5
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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/jm00018a005
CHEMBL5090946 215285 None 0 Human Functional pEC50 = 8.9 8.9 -12 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263822 210590 None 0 Human Functional pEC50 = 8.9 8.9 5 4
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL5087859 215123 None 0 Human Functional pEC50 = 8.9 8.9 4 3
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845450 138469 None 0 Human Functional pEC50 = 8.9 8.9 -28 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 138469 None 0 Human Functional pEC50 = 8.9 8.9 -28 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
118722931 116234 None 0 Mouse Functional pEC50 = 8.9 8.9 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358540 116234 None 0 Mouse Functional pEC50 = 8.9 8.9 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
16132144 209279 None 36 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
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 10.1016/s0960-894x(03)00796-0
16133793 209279 None 36 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
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 10.1016/s0960-894x(03)00796-0
44273719 209279 None 36 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
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 10.1016/s0960-894x(03)00796-0
CHEMBL214332 209279 None 36 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
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 10.1016/s0960-894x(03)00796-0
CHEMBL5083551 214869 None 0 Human Functional pEC50 = 8.8 8.8 -25 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3600920 211823 None 0 Human Functional pEC50 = 8.8 8.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 55 Human Functional pEC50 = 8.8 8.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 55 Human Functional pEC50 = 8.8 8.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.8 8.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
118722927 116231 None 0 Mouse Functional pEC50 = 8.8 8.8 -8 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=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)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358536 116231 None 0 Mouse Functional pEC50 = 8.8 8.8 -8 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=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)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL439691 213848 None 0 Human Functional pEC50 = 8.8 8.8 5 3
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438030 213744 None 0 Human Functional pEC50 = 8.8 8.8 21 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL267900 210737 None 0 Human Functional pEC50 = 8.8 8.8 -5 2
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL1688107 208834 None 0 Mouse Functional pEC50 = 8.8 8.8 -8 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
145971389 164633 None 0 Human Functional pEC50 = 8.7 8.7 2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164633 None 0 Human Functional pEC50 = 8.7 8.7 2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
1323 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
92432 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL393075 212462 None 0 Human Functional pEC50 = 8.7 8.7 -6 4
Effect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None CCCC[C@H](N)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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
1323 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
1323 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
145973975 164657 None 0 Human Functional pEC50 = 8.7 8.7 11 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164657 None 0 Human Functional pEC50 = 8.7 8.7 11 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
92432 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.7 8.7 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
CHEMBL3752534 212216 None 1 Human Functional pEC50 = 8.7 8.7 25 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
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]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
118722940 116241 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358548 116241 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358537 211568 None 0 Mouse Functional pEC50 = 8.7 8.7 -7 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
44416106 141446 None 0 Human Functional pEC50 = 8 8.0 -19 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 141446 None 0 Human Functional pEC50 = 8 8.0 -19 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44413830 77950 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209622 77950 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
155549760 173877 None 0 Mouse Functional pEC50 = 8 8.0 -25 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539621 173877 None 0 Mouse Functional pEC50 = 8 8.0 -25 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
127047475 139749 None 0 Mouse Functional pEC50 = 8 8.0 -60 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
132991507 139749 None 0 Mouse Functional pEC50 = 8 8.0 -60 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798421 139749 None 0 Mouse Functional pEC50 = 8 8.0 -60 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
16132144 209279 None 36 Mouse Functional pEC50 = 8.0 8.0 -2 8
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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 10.1016/j.bmcl.2009.07.025
16133793 209279 None 36 Mouse Functional pEC50 = 8.0 8.0 -2 8
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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 10.1016/j.bmcl.2009.07.025
44273719 209279 None 36 Mouse Functional pEC50 = 8.0 8.0 -2 8
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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 10.1016/j.bmcl.2009.07.025
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 8.0 8.0 -2 8
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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 10.1016/j.bmcl.2009.07.025
24774358 154904 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL400866 154904 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
155565321 175576 None 0 Mouse Functional pEC50 = 7 7.0 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4579448 175576 None 0 Mouse Functional pEC50 = 7 7.0 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155567399 175966 None 0 Mouse Functional pEC50 = 7 7.0 -21 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4588429 175966 None 0 Mouse Functional pEC50 = 7 7.0 -21 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL320157 211226 None 0 Mouse Functional pEC50 = 7 7.0 -1 4
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 assayAgonist 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
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
137638725 156979 None 0 Human Functional pEC50 = 6 6.0 -38 3
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4073016 156979 None 0 Human Functional pEC50 = 6 6.0 -38 3
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137660671 159218 None 0 Human Functional pEC50 = 6 6.0 -1071 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 159218 None 0 Human Functional pEC50 = 6 6.0 -1071 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL411359 212879 None 0 Human Functional pEC50 = 6 6.0 -4 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
155566074 175734 None 0 Mouse Functional pEC50 = 5 5.0 -33 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582914 175734 None 0 Mouse Functional pEC50 = 5 5.0 -33 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 722 15 8 7 -1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44305763 203086 None 0 Mouse Functional pEC50 = 4 4.0 -5 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL63850 203086 None 0 Mouse Functional pEC50 = 4 4.0 -5 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
44305704 203337 None 0 Mouse Functional pEC50 = 4 4.0 -4 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL64954 203337 None 0 Mouse Functional pEC50 = 4 4.0 -4 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44441645 94127 None 0 Human Functional pEC50 = 6 6.0 -93 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 94127 None 0 Human Functional pEC50 = 6 6.0 -93 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44394660 67054 None 0 Human Functional pEC50 = 6.0 6.0 -70 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL187167 67054 None 0 Human Functional pEC50 = 6.0 6.0 -70 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394654 123973 None 0 Human Functional pEC50 = 6.0 6.0 -26 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL362879 123973 None 0 Human Functional pEC50 = 6.0 6.0 -26 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11787684 70274 None 0 Mouse Functional pEC50 = 7.0 7.0 -36 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL194217 70274 None 0 Mouse Functional pEC50 = 7.0 7.0 -36 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
25132866 172611 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL449131 172611 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL2323791 209517 None 0 Mouse Functional pEC50 = 5.0 5.0 -9 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
155556047 174497 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4554828 174497 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4299612 213594 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CC(=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)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/acs.jmedchem.5b01894
46885761 8028 None 0 Human Functional pEC50 = 5.0 5.0 -173 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL1090813 8028 None 0 Human Functional pEC50 = 5.0 5.0 -173 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
71457994 78579 None 0 Mouse Functional pEC50 = 5.0 5.0 -26 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
CHEMBL2112213 78579 None 0 Mouse Functional pEC50 = 5.0 5.0 -26 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 441 8 5 3 3.7 NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(03)00318-4
25133556 188849 None 0 Human Functional pEC50 = 7.0 7.0 -83 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 188849 None 0 Human Functional pEC50 = 7.0 7.0 -83 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
122184635 122434 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122434 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
162673830 183159 None 0 Mouse Functional pEC50 = 8.0 8.0 -47 3
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 assayAgonist 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
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4795352 183159 None 0 Mouse Functional pEC50 = 8.0 8.0 -47 3
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 assayAgonist 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
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL2371712 210109 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 8.0 8.0 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5091236 215299 None 0 Human Functional pEC50 = 8.0 8.0 -102 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
90643803 111743 None 0 Mouse Functional pEC50 = 7.9 7.9 -26 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111743 None 0 Mouse Functional pEC50 = 7.9 7.9 -26 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155556954 174548 None 0 Mouse Functional pEC50 = 7.0 7.0 -363 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4556149 174548 None 0 Mouse Functional pEC50 = 7.0 7.0 -363 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162662213 181496 None 0 Mouse Functional pEC50 = 7.0 7.0 -2 3
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 assayAgonist 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
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4764827 181496 None 0 Mouse Functional pEC50 = 7.0 7.0 -2 3
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 assayAgonist 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
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162661724 181535 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 3
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 assayAgonist 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
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4765199 181535 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 3
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 assayAgonist 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
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
25128751 173584 None 0 Human Functional pEC50 = 6.0 6.0 -29 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 173584 None 0 Human Functional pEC50 = 6.0 6.0 -29 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
137642664 158080 None 0 Mouse Functional pEC50 = 6.0 6.0 -12 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4086346 158080 None 0 Mouse Functional pEC50 = 6.0 6.0 -12 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 772 18 9 7 -0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
155551195 173942 None 0 Mouse Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4541098 173942 None 0 Mouse Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
71459938 78981 None 0 Human Functional pEC50 = 6.0 6.0 -19 4
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 78981 None 0 Human Functional pEC50 = 6.0 6.0 -19 4
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
25128749 178470 None 0 Human Functional pEC50 = 7.0 7.0 -37 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 178470 None 0 Human Functional pEC50 = 7.0 7.0 -37 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL3601426 211826 None 0 Human Functional pEC50 = 6.0 6.0 -24 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
11847001 80228 None 0 Human Functional pEC50 = 6.0 6.0 -125 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 80228 None 0 Human Functional pEC50 = 6.0 6.0 -125 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44441641 94301 None 0 Human Functional pEC50 = 6.9 6.9 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 94301 None 0 Human Functional pEC50 = 6.9 6.9 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
145989222 167280 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 167280 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
11328898 7960 None 22 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 7960 None 22 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1204059 7960 None 22 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
46885972 8119 None 0 Human Functional pEC50 = 4.9 4.9 -165 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1091631 8119 None 0 Human Functional pEC50 = 4.9 4.9 -165 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
11845630 139514 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 139514 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL589515 215800 None 0 Mouse Functional pEC50 = 4.9 4.9 -169 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmc.2009.12.010
25129453 171766 None 0 Human Functional pEC50 = 7.9 7.9 -15 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 171766 None 0 Human Functional pEC50 = 7.9 7.9 -15 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
145966490 164362 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 164362 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 7.9 7.9 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2370967 209970 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
145980719 166496 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 166496 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44322957 206211 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 206211 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408189 168879 None 0 Human Functional pEC50 = 5.9 5.9 -107 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168879 None 0 Human Functional pEC50 = 5.9 5.9 -107 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
16132144 209279 None 36 Mouse Functional pEC50 = 5.9 5.9 -2 8
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
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 10.1016/s0960-894x(03)00318-4
16133793 209279 None 36 Mouse Functional pEC50 = 5.9 5.9 -2 8
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
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 10.1016/s0960-894x(03)00318-4
44273719 209279 None 36 Mouse Functional pEC50 = 5.9 5.9 -2 8
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
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 10.1016/s0960-894x(03)00318-4
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 5.9 5.9 -2 8
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
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 10.1016/s0960-894x(03)00318-4
44413881 137593 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 137593 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
137635422 155910 None 0 Human Functional pEC50 = 6.9 6.9 -30 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 155910 None 0 Human Functional pEC50 = 6.9 6.9 -30 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL510687 215587 None 0 Mouse Functional pEC50 = 5.9 5.9 -141 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL105113 208466 None 0 Mouse Functional pEC50 = 4.9 4.9 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 6.9 6.9 -35 8
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=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(N)=O 10.1021/jm800291b
15603023 97964 None 0 Mouse Functional pEC50 = 5.9 5.9 -630 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL272660 97964 None 0 Mouse Functional pEC50 = 5.9 5.9 -630 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL5093939 215458 None 0 Human Functional pEC50 = 6.9 6.9 -169 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2310901 209498 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44322958 107012 None 0 Human Functional pEC50 = 7.9 7.9 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 107012 None 0 Human Functional pEC50 = 7.9 7.9 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL3600843 211820 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5076315 214428 None 0 Human Functional pEC50 = 7.9 7.9 -8 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL501592 214141 None 0 Human Functional pEC50 = 6.9 6.9 -37 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
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]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44322986 106097 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 106097 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
155567887 176048 None 0 Mouse Functional pEC50 = 5.9 5.9 -4 4
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 assayAgonist 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
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4590532 176048 None 0 Mouse Functional pEC50 = 5.9 5.9 -4 4
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 assayAgonist 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
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
137640475 157087 None 0 Mouse Functional pEC50 = 4.9 4.9 -29 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4074368 157087 None 0 Mouse Functional pEC50 = 4.9 4.9 -29 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 870 16 7 6 2.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
1338 3807 None 43 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 43 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 43 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
11308957 69393 None 0 Mouse Functional pEC50 = 6.9 6.9 -64 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL193151 69393 None 0 Mouse Functional pEC50 = 6.9 6.9 -64 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44394093 127239 None 0 Human Functional pEC50 = 5.9 5.9 -8 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365825 127239 None 0 Human Functional pEC50 = 5.9 5.9 -8 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL217584 209377 None 0 Human Functional pEC50 = 6.9 6.9 -74 3
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 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](C)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)NC1=O 10.1021/jm960845e
CHEMBL3350327 211470 None 0 Mouse Functional pEC50 = 4.9 4.9 -1 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
11846673 79994 None 0 Human Functional pEC50 = 5.9 5.9 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 79994 None 0 Human Functional pEC50 = 5.9 5.9 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
11491374 67620 None 0 Mouse Functional pEC50 = 6.9 6.9 -147 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL190366 67620 None 0 Mouse Functional pEC50 = 6.9 6.9 -147 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL500743 214124 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
162649653 180100 None 0 Mouse Functional pEC50 = 7.9 7.9 -23 3
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 assayAgonist 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
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4748317 180100 None 0 Mouse Functional pEC50 = 7.9 7.9 -23 3
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 assayAgonist 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
ChEMBL 753 18 10 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162661397 181526 None 0 Mouse Functional pEC50 = 7.9 7.9 -2 4
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 assayAgonist 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
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4765156 181526 None 0 Mouse Functional pEC50 = 7.9 7.9 -2 4
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 assayAgonist 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
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
162672755 183090 None 0 Mouse Functional pEC50 = 7.9 7.9 -35 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 183090 None 0 Mouse Functional pEC50 = 7.9 7.9 -35 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
44394786 124080 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363271 124080 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL2096759 209208 None 0 Human Functional pEC50 = 6.9 6.9 -21 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
122184914 122559 None 0 Human Functional pEC50 = 5.9 5.9 -69 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122559 None 0 Human Functional pEC50 = 5.9 5.9 -69 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44422999 168855 None 0 Human Functional pEC50 = 5.9 5.9 -446 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 168855 None 0 Human Functional pEC50 = 5.9 5.9 -446 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
155538472 173251 None 0 Mouse Functional pEC50 = 5.9 5.9 -10 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4524668 173251 None 0 Mouse Functional pEC50 = 5.9 5.9 -10 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
1338 3807 None 43 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 3807 None 43 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 3807 None 43 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
137634090 156299 None 0 Mouse Functional pEC50 = 4.9 4.9 -10 6
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 156299 None 0 Mouse Functional pEC50 = 4.9 4.9 -10 6
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
137635701 156037 None 0 Mouse Functional pEC50 = 4.9 4.9 -1 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4062425 156037 None 0 Mouse Functional pEC50 = 4.9 4.9 -1 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
162669632 182565 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182565 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44416152 81098 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 81098 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394657 127464 None 0 Human Functional pEC50 = 5.8 5.8 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL366040 127464 None 0 Human Functional pEC50 = 5.8 5.8 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394583 122345 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359927 122345 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44456964 156690 None 0 Mouse Functional pEC50 = 5.8 5.8 -81 4
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL406985 156690 None 0 Mouse Functional pEC50 = 5.8 5.8 -81 4
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
25129105 177019 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 177019 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
44413968 80229 None 0 Human Functional pEC50 = 5.8 5.8 -77 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 80229 None 0 Human Functional pEC50 = 5.8 5.8 -77 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
137658158 159717 None 0 Human Functional pEC50 = 5.8 5.8 -26 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159717 None 0 Human Functional pEC50 = 5.8 5.8 -26 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
9849434 176930 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL462044 176930 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL184968 209052 None 0 Human Functional pEC50 = 5.8 5.8 -11 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CCC(=O)OC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25133907 176724 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 176724 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44413914 139518 None 0 Human Functional pEC50 = 7.8 7.8 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 139518 None 0 Human Functional pEC50 = 7.8 7.8 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
155555217 174337 None 0 Mouse Functional pEC50 = 7.8 7.8 -9 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550976 174337 None 0 Mouse Functional pEC50 = 7.8 7.8 -9 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL307457 210981 None 0 Mouse Functional pEC50 = 7.8 7.8 -36 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL5087814 215119 None 0 Human Functional pEC50 = 7.8 7.8 -12 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44577516 172874 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL451535 172874 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
162664463 182190 None 0 Mouse Functional pEC50 = 6.8 6.8 -4 3
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 assayAgonist 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
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4782762 182190 None 0 Mouse Functional pEC50 = 6.8 6.8 -4 3
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 assayAgonist 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
ChEMBL 706 15 6 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
11273288 12960 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 12960 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL538567 12960 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL2370965 209968 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
137657151 159556 None 0 Mouse Functional pEC50 = 5.8 5.8 -3 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102613 159556 None 0 Mouse Functional pEC50 = 5.8 5.8 -3 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL50056 214119 None 2 Mouse Functional pEC50 = 5.8 5.8 -138 7
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 assayAgonist 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
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 5.8 5.8 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL320157 211226 None 0 Mouse Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
162672691 183201 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183201 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
11423083 96839 None 0 Mouse Functional pEC50 = 6.8 6.8 -154 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL265236 96839 None 0 Mouse Functional pEC50 = 6.8 6.8 -154 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
162672691 183201 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183201 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 6.8 6.8 -35 8
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=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(N)=O 10.1021/jm010524p
44448590 95599 None 0 Human Functional pEC50 = 6.8 6.8 -93 3
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95599 None 0 Human Functional pEC50 = 6.8 6.8 -93 3
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600842 211819 None 0 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
132180598 157849 None 0 Mouse Functional pEC50 = 7.8 7.8 -181 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4083717 157849 None 0 Mouse Functional pEC50 = 7.8 7.8 -181 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL5077144 214485 None 0 Human Functional pEC50 = 7.8 7.8 -38 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 209279 None 36 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
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/acs.jmedchem.7b00353
16133793 209279 None 36 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
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/acs.jmedchem.7b00353
44273719 209279 None 36 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
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/acs.jmedchem.7b00353
CHEMBL214332 209279 None 36 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
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/acs.jmedchem.7b00353
1323 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
137637026 155925 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 155925 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
1338 3807 None 43 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 43 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 43 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
137639815 156802 None 0 Mouse Functional pEC50 = 6.8 6.8 -7 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4071063 156802 None 0 Mouse Functional pEC50 = 6.8 6.8 -7 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 6.8 6.8 -35 8
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
ChEMBL None None None CC(=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(N)=O 10.1016/j.bmcl.2003.08.078
44322923 206546 None 0 Human Functional pEC50 = 6.8 6.8 -19 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 206546 None 0 Human Functional pEC50 = 6.8 6.8 -19 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10325955 165271 None 0 Human Functional pEC50 = 5.8 5.8 -112 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 165271 None 0 Human Functional pEC50 = 5.8 5.8 -112 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
155562846 175170 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4570356 175170 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 564 13 5 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL184326 209049 None 0 Human Functional pEC50 = 5.8 5.8 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None COP(=S)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC 10.1016/j.bmcl.2004.07.046
CHEMBL3350396 211479 None 0 Human Functional pEC50 = 6.8 6.8 -281 4
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 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](C)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)NC1=O 10.1021/jm960845e
137662147 159379 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 159379 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
122184575 122427 None 0 Human Functional pEC50 = 6.8 6.8 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 122427 None 0 Human Functional pEC50 = 6.8 6.8 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
168272615 190387 None 0 Human Functional pEC50 = 6.8 6.8 -31 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 190387 None 0 Human Functional pEC50 = 6.8 6.8 -31 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44416060 81318 None 0 Human Functional pEC50 = 6.8 6.8 -102 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 81318 None 0 Human Functional pEC50 = 6.8 6.8 -102 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394658 168337 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434329 168337 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL500516 214117 None 0 Mouse Functional pEC50 = 4.8 4.8 -74 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL364359 211922 None 0 Human Functional pEC50 = 5.8 5.8 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NS(=O)(=O)C(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL195468 209102 None 0 Mouse Functional pEC50 = 6.8 6.8 -53 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
45487297 197101 None 0 Mouse Functional pEC50 = 4.8 4.8 -33 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567634 197101 None 0 Mouse Functional pEC50 = 4.8 4.8 -33 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 613 17 8 6 0.7 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
162665450 182296 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182296 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1323 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 55 Human Functional pEC50 = 7.8 7.8 -58 8
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
44323031 168078 None 0 Human Functional pEC50 = 7.8 7.8 -33 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 168078 None 0 Human Functional pEC50 = 7.8 7.8 -33 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075712 214394 None 0 Human Functional pEC50 = 7.8 7.8 -125 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44394694 66312 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184895 66312 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183733 209047 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL50056 214119 None 2 Human Functional pEC50 = 6.8 6.8 -15 7
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL203602 209160 None 0 Human Functional pEC50 = 5.8 5.8 -1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
CHEMBL2370968 209971 None 0 Human Functional pEC50 = 5.8 5.8 -63 4
Agonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
11753695 8393 None 7 Mouse Functional pEC50 = 5.8 5.8 -851 8
Agonist activity at mouse MC3 receptorAgonist activity at mouse MC3 receptor
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1093304 8393 None 7 Mouse Functional pEC50 = 5.8 5.8 -851 8
Agonist activity at mouse MC3 receptorAgonist activity at mouse MC3 receptor
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
44305770 202794 None 0 Mouse Functional pEC50 = 5.8 5.8 1 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL62228 202794 None 0 Mouse Functional pEC50 = 5.8 5.8 1 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL2370968 209971 None 0 Human Functional pEC50 = 5.8 5.8 -63 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 6.8 6.8 -35 8
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None CC(=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(N)=O 10.1021/jm0490843
162665450 182296 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182296 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL302703 210914 None 0 Mouse Functional pEC50 = 5.8 5.8 -5 5
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL361252 211834 None 0 Human Functional pEC50 = 6.8 6.8 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CN(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11847312 79762 None 0 Human Functional pEC50 = 5.8 5.8 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 79762 None 0 Human Functional pEC50 = 5.8 5.8 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
122184638 122437 None 0 Human Functional pEC50 = 5.8 5.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 122437 None 0 Human Functional pEC50 = 5.8 5.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5092761 215388 None 0 Human Functional pEC50 = 7.7 7.7 -281 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2323786 209512 None 0 Mouse Functional pEC50 = 6.8 6.8 -12 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
10077258 15031 None 0 Human Functional pEC50 = 5.8 5.8 -158 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15031 None 0 Human Functional pEC50 = 5.8 5.8 -158 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
11226756 119974 None 0 Human Functional pEC50 = 5.8 5.8 -251 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 119974 None 0 Human Functional pEC50 = 5.8 5.8 -251 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
155538874 172790 None 0 Mouse Functional pEC50 = 4.8 4.8 -10 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4513460 172790 None 0 Mouse Functional pEC50 = 4.8 4.8 -10 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 713 16 8 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
122184636 122435 None 0 Human Functional pEC50 = 5.7 5.7 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 122435 None 0 Human Functional pEC50 = 5.7 5.7 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2323799 209525 None 0 Mouse Functional pEC50 = 5.7 5.7 -120 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
145976444 163963 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[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/acs.jmedchem.8b00488
CHEMBL4207858 163963 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[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/acs.jmedchem.8b00488
CHEMBL3287327 211310 None 0 Mouse Functional pEC50 = 7.7 7.7 -7 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL438235 213759 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
137638778 156758 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 156758 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL5090670 215277 None 0 Human Functional pEC50 = 7.7 7.7 -18 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2323793 209519 None 0 Mouse Functional pEC50 = 6.7 6.7 -25 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
168277258 190710 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 190710 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL2323790 209516 None 0 Mouse Functional pEC50 = 5.7 5.7 -60 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
155555947 174512 None 0 Mouse Functional pEC50 = 4.7 4.7 -147 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4555150 174512 None 0 Mouse Functional pEC50 = 4.7 4.7 -147 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 592 14 7 6 -0.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
168274920 190263 None 0 Human Functional pEC50 = 6.7 6.7 -66 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 190263 None 0 Human Functional pEC50 = 6.7 6.7 -66 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 6.7 6.7 -35 8
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=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(N)=O 10.1021/jm010061n
CHEMBL3601431 211827 None 0 Human Functional pEC50 = 5.7 5.7 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
45487298 197342 None 0 Mouse Functional pEC50 = 4.7 4.7 -25 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568965 197342 None 0 Mouse Functional pEC50 = 4.7 4.7 -25 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
44415919 141588 None 0 Human Functional pEC50 = 8.7 8.7 4 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 141588 None 0 Human Functional pEC50 = 8.7 8.7 4 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL503229 214163 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=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)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
44577510 188735 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188735 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL1688107 208834 None 0 Mouse Functional pEC50 = 8.7 8.7 -8 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL443071 213920 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 8.7 8.7 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
16132144 209279 None 36 Mouse Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
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/jm701303z
16133793 209279 None 36 Mouse Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
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/jm701303z
44273719 209279 None 36 Mouse Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
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/jm701303z
CHEMBL214332 209279 None 36 Mouse Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
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/jm701303z
CHEMBL5087839 215120 None 0 Human Functional pEC50 = 8.7 8.7 -2 3
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3358533 211567 None 0 Mouse Functional pEC50 = 8.7 8.7 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=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)N[C@@H](CCCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
118722932 115518 None 0 Mouse Functional pEC50 = 8.6 8.6 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)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)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3352878 115518 None 0 Mouse Functional pEC50 = 8.6 8.6 -10 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)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)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
10408 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 28 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
1323 2688 None 55 Human Functional pEC50 = 8.6 8.6 -58 8
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 55 Human Functional pEC50 = 8.6 8.6 -58 8
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.6 8.6 -58 8
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL3358542 211569 None 0 Mouse Functional pEC50 = 8.6 8.6 -7 3
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(C)=O)C(N)=O 10.1021/jm501027w
168278271 191115 None 0 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 191115 None 0 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16132144 209279 None 36 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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/jm9017866
16133793 209279 None 36 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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/jm9017866
44273719 209279 None 36 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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/jm9017866
CHEMBL214332 209279 None 36 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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/jm9017866
44348200 160196 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 160196 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL266417 210683 None 0 Human Functional pEC50 = 8.6 8.6 -83 6
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL4299619 213595 None 0 Mouse Functional pEC50 = 7.7 7.7 -66 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CC(=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)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
137660993 159447 None 0 Human Functional pEC50 = 7.7 7.7 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 159447 None 0 Human Functional pEC50 = 7.7 7.7 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL2323785 209511 None 0 Mouse Functional pEC50 = 6.7 6.7 -32 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
118735102 118802 None 0 Human Functional pEC50 = 5.7 5.7 -53 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 118802 None 0 Human Functional pEC50 = 5.7 5.7 -53 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
10257242 15030 None 0 Human Functional pEC50 = 5.7 5.7 -112 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 15030 None 0 Human Functional pEC50 = 5.7 5.7 -112 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
155548791 173730 None 0 Mouse Functional pEC50 = 5.7 5.7 -25 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4536340 173730 None 0 Mouse Functional pEC50 = 5.7 5.7 -25 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 664 14 6 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
164627491 186503 None 0 Mouse Functional pEC50 = 5.7 5.7 3 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4877442 186503 None 0 Mouse Functional pEC50 = 5.7 5.7 3 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 11 3 3 5.8 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
9960253 116949 None 0 Human Functional pEC50 = 5.7 5.7 -25 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 116949 None 0 Human Functional pEC50 = 5.7 5.7 -25 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44409240 74434 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 74434 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44415972 79883 None 0 Human Functional pEC50 = 4.7 4.7 -141 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 79883 None 0 Human Functional pEC50 = 4.7 4.7 -141 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
44415956 141956 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 141956 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44409240 74434 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 74434 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
44413832 78065 None 0 Human Functional pEC50 = 4.7 4.7 -38 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210009 78065 None 0 Human Functional pEC50 = 4.7 4.7 -38 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
11845444 80067 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 80067 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413969 80230 None 0 Human Functional pEC50 = 4.7 4.7 -44 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 80230 None 0 Human Functional pEC50 = 4.7 4.7 -44 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44413970 139015 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 139015 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44415956 141956 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 141956 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44394785 124040 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363061 124040 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137631599 156526 None 0 Human Functional pEC50 = 6.7 6.7 -50 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156526 None 0 Human Functional pEC50 = 6.7 6.7 -50 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL319871 211224 None 0 Mouse Functional pEC50 = 5.7 5.7 -177 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44457043 97612 None 0 Mouse Functional pEC50 = 4.7 4.7 -204 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL270923 97612 None 0 Mouse Functional pEC50 = 4.7 4.7 -204 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
45487415 197439 None 0 Mouse Functional pEC50 = 4.7 4.7 -245 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569697 197439 None 0 Mouse Functional pEC50 = 4.7 4.7 -245 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
11845276 80053 None 0 Human Functional pEC50 = 5.7 5.7 -7 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 80053 None 0 Human Functional pEC50 = 5.7 5.7 -7 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
44394695 123158 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361253 123158 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
155563222 175291 None 0 Mouse Functional pEC50 = 7.7 7.7 -69 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4572994 175291 None 0 Mouse Functional pEC50 = 7.7 7.7 -69 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL3287329 211311 None 0 Mouse Functional pEC50 = 7.7 7.7 -4 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155558348 175036 None 0 Mouse Functional pEC50 = 6.7 6.7 -11 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567480 175036 None 0 Mouse Functional pEC50 = 6.7 6.7 -11 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155562237 175709 None 0 Mouse Functional pEC50 = 6.7 6.7 -104 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582276 175709 None 0 Mouse Functional pEC50 = 6.7 6.7 -104 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
164623811 185900 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868636 185900 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL427629 213357 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
137655905 158828 None 0 Human Functional pEC50 = 5.7 5.7 -51 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158828 None 0 Human Functional pEC50 = 5.7 5.7 -51 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44413828 139293 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 139293 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
25132864 172602 None 0 Human Functional pEC50 = 6.7 6.7 -42 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 172602 None 0 Human Functional pEC50 = 6.7 6.7 -42 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
162672755 183090 None 0 Mouse Functional pEC50 = 7.7 7.7 -35 3
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 assayAgonist 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
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4794484 183090 None 0 Mouse Functional pEC50 = 7.7 7.7 -35 3
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 assayAgonist 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
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
90643805 111745 None 0 Mouse Functional pEC50 = 7.7 7.7 -7 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111745 None 0 Mouse Functional pEC50 = 7.7 7.7 -7 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
127047853 139993 None 0 Mouse Functional pEC50 = 7.6 7.6 -123 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799955 139993 None 0 Mouse Functional pEC50 = 7.6 7.6 -123 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
164610489 184555 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 10 4 4 5.8 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4848322 184555 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 10 4 4 5.8 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
11239907 133127 None 0 Mouse Functional pEC50 = 6.7 6.7 -380 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL370261 133127 None 0 Mouse Functional pEC50 = 6.7 6.7 -380 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
137634090 156299 None 0 Human Functional pEC50 = 4.7 4.7 -15 6
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 156299 None 0 Human Functional pEC50 = 4.7 4.7 -15 6
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL2323529 209510 None 0 Mouse Functional pEC50 = 5.7 5.7 -28 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2369131 209593 None 0 Mouse Functional pEC50 = 4.7 4.7 -6 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL5081077 214717 None 0 Human Functional pEC50 = 7.6 7.6 -29 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
9867330 97841 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 97841 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL2323787 209513 None 0 Mouse Functional pEC50 = 6.6 6.6 -11 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44441684 94131 None 0 Human Functional pEC50 = 6.6 6.6 -28 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 94131 None 0 Human Functional pEC50 = 6.6 6.6 -28 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
44323015 111433 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 111433 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
137657206 159671 None 0 Mouse Functional pEC50 = 5.6 5.6 1 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103985 159671 None 0 Mouse Functional pEC50 = 5.6 5.6 1 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 914 19 8 7 3.9 CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
11845272 80358 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 80358 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44457002 97572 None 0 Mouse Functional pEC50 = 4.6 4.6 -5 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
CHEMBL270691 97572 None 0 Mouse Functional pEC50 = 4.6 4.6 -5 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 440 4 1 2 5.4 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccc3ccccc3c2)c2cc(Cl)ccc21 10.1021/jm701303z
44394626 65784 None 0 Human Functional pEC50 = 5.6 5.6 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183476 65784 None 0 Human Functional pEC50 = 5.6 5.6 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25132524 176758 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 176758 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
122184637 122436 None 0 Human Functional pEC50 = 5.6 5.6 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 122436 None 0 Human Functional pEC50 = 5.6 5.6 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL448536 213959 None 0 Mouse Functional pEC50 = 6.6 6.6 -85 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164619151 185554 None 0 Mouse Functional pEC50 = 6.6 6.6 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4863206 185554 None 0 Mouse Functional pEC50 = 6.6 6.6 1 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 610 11 4 4 5.5 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL409636 212773 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)NC1=O 10.1021/jm030119t
44397461 126227 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 126227 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2370963 209966 None 0 Human Functional pEC50 = 5.6 5.6 -85 2
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44441685 94132 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249322 94132 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
45487294 196813 None 0 Mouse Functional pEC50 = 4.6 4.6 -23 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565688 196813 None 0 Mouse Functional pEC50 = 4.6 4.6 -23 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 601 17 8 6 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
118735101 118801 None 0 Human Functional pEC50 = 5.6 5.6 -64 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118801 None 0 Human Functional pEC50 = 5.6 5.6 -64 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL433296 213636 None 0 Mouse Functional pEC50 = 5.6 5.6 -39 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
168295131 192242 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 192242 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11845440 138672 None 0 Human Functional pEC50 = 5.6 5.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL377778 138672 None 0 Human Functional pEC50 = 5.6 5.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL50056 214119 None 2 Human Functional pEC50 = 6.6 6.6 -15 7
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm060384p
1338 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 43 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44448660 94973 None 0 Human Functional pEC50 = 6.6 6.6 -691 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 94973 None 0 Human Functional pEC50 = 6.6 6.6 -691 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44569175 188822 None 0 Human Functional pEC50 = 7.6 7.6 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 188822 None 0 Human Functional pEC50 = 7.6 7.6 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
1323 2688 None 55 Human Functional pEC50 = 7.6 7.6 -58 8
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
92432 2688 None 55 Human Functional pEC50 = 7.6 7.6 -58 8
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL430239 2688 None 55 Human Functional pEC50 = 7.6 7.6 -58 8
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL410795 212842 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL370254 212166 None 3 Mouse Functional pEC50 = 6.6 6.6 -91 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm0490843
49862425 15060 None 0 Human Functional pEC50 = 5.6 5.6 -91 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 15060 None 0 Human Functional pEC50 = 5.6 5.6 -91 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL524861 215623 None 0 Human Functional pEC50 = 5.6 5.6 -17 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
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](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
137640715 157003 None 0 Mouse Functional pEC50 = 5.6 5.6 -34 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4073316 157003 None 0 Mouse Functional pEC50 = 5.6 5.6 -34 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
137649203 157508 None 0 Mouse Functional pEC50 = 5.6 5.6 -1 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079721 157508 None 0 Mouse Functional pEC50 = 5.6 5.6 -1 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 894 18 8 8 3.5 CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
145990599 166855 None 0 Human Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 166855 None 0 Human Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL2323798 209524 None 0 Mouse Functional pEC50 = 5.6 5.6 -85 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCN)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
145980198 166686 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4282109 166686 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
45487299 197375 None 0 Mouse Functional pEC50 = 4.6 4.6 -48 2
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 661 19 8 8 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCCc1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569222 197375 None 0 Mouse Functional pEC50 = 4.6 4.6 -48 2
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 661 19 8 8 0.5 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCCc1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
155544214 173331 None 0 Mouse Functional pEC50 = 7.6 7.6 -8 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 797 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4526652 173331 None 0 Mouse Functional pEC50 = 7.6 7.6 -8 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 797 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
45487403 197435 None 0 Mouse Functional pEC50 = 7.6 7.6 -2630 5
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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 197435 None 0 Mouse Functional pEC50 = 7.6 7.6 -2630 5
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
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
11846669 80277 None 0 Human Functional pEC50 = 6.6 6.6 -18 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 80277 None 0 Human Functional pEC50 = 6.6 6.6 -18 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
137656489 159710 None 0 Mouse Functional pEC50 = 6.6 6.6 -14 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4104402 159710 None 0 Mouse Functional pEC50 = 6.6 6.6 -14 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
10886436 119157 None 0 Mouse Functional pEC50 = 6.6 6.6 -537 5
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
CHEMBL342954 119157 None 0 Mouse Functional pEC50 = 6.6 6.6 -537 5
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
44441644 154838 None 0 Human Functional pEC50 = 6.6 6.6 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 154838 None 0 Human Functional pEC50 = 6.6 6.6 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL434357 213652 None 0 Human Functional pEC50 = 5.6 5.6 -19 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None COP(=O)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC 10.1016/j.bmcl.2004.07.046
44413880 77946 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 77946 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
11263053 68020 None 0 Mouse Functional pEC50 = 6.6 6.6 -363 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191304 68020 None 0 Mouse Functional pEC50 = 6.6 6.6 -363 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
137659790 159322 None 0 Human Functional pEC50 = 5.6 5.6 -11 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 159322 None 0 Human Functional pEC50 = 5.6 5.6 -11 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137653925 158607 None 0 Human Functional pEC50 = 4.6 4.6 -64 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 158607 None 0 Human Functional pEC50 = 4.6 4.6 -64 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL427205 213352 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
24774602 168931 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 168931 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3799094 212268 None 0 Mouse Functional pEC50 = 7.6 7.6 -97 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL2115441 209268 None 0 Human Functional pEC50 = 7.6 7.6 -144 4
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 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](C)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)NC1=O 10.1021/jm960845e
155549385 173805 None 0 Mouse Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4538225 173805 None 0 Mouse Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
25132525 176725 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 176725 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
145971673 164698 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217191 164698 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44400428 125677 None 0 Mouse Functional pEC50 = 6.6 6.6 -331 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL364726 125677 None 0 Mouse Functional pEC50 = 6.6 6.6 -331 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44323032 206604 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 206604 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162672255 182871 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182871 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL383250 212312 None 0 Human Functional pEC50 = 5.6 5.6 -18 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
164626394 186591 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 11 3 3 6.5 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4878558 186591 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 11 3 3 6.5 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
45487406 196894 None 0 Mouse Functional pEC50 = 4.6 4.6 -24 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566150 196894 None 0 Mouse Functional pEC50 = 4.6 4.6 -24 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
137659790 159322 None 0 Human Functional pEC50 = 6.6 6.6 -11 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 159322 None 0 Human Functional pEC50 = 6.6 6.6 -11 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44413829 78066 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 78066 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44445082 154302 None 0 Human Functional pEC50 = 7.5 7.5 6 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 154302 None 0 Human Functional pEC50 = 7.5 7.5 6 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
162672255 182871 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182871 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44310344 97329 None 0 Mouse Functional pEC50 = 7.5 7.5 -186 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
77231883 97329 None 0 Mouse Functional pEC50 = 7.5 7.5 -186 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL269274 97329 None 0 Mouse Functional pEC50 = 7.5 7.5 -186 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
137656521 159744 None 0 Human Functional pEC50 = 6.5 6.5 -12 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 159744 None 0 Human Functional pEC50 = 6.5 6.5 -12 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44391927 13991 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 13991 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL3216393 13991 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
168296647 192475 None 0 Human Functional pEC50 = 6.5 6.5 -158 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 192475 None 0 Human Functional pEC50 = 6.5 6.5 -158 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44441648 154691 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 154691 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44413842 138377 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 138377 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44394624 97016 None 0 Human Functional pEC50 = 8.5 8.5 -60 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL266665 97016 None 0 Human Functional pEC50 = 8.5 8.5 -60 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL410404 212819 None 0 Rat Functional pEC50 = 8.5 8.5 -25 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1323 2688 None 55 Human Functional pEC50 = 8.5 8.5 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 55 Human Functional pEC50 = 8.5 8.5 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.5 8.5 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
118722935 116236 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358543 116236 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
145966716 164305 None 0 Human Functional pEC50 = 8.5 8.5 18 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 164305 None 0 Human Functional pEC50 = 8.5 8.5 18 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
118722925 116229 None 0 Mouse Functional pEC50 = 8.5 8.5 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)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)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358534 116229 None 0 Mouse Functional pEC50 = 8.5 8.5 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)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)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL5094168 215479 None 0 Human Functional pEC50 = 8.5 8.5 -42 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
118722929 116232 None 0 Mouse Functional pEC50 = 8.4 8.4 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358538 116232 None 0 Mouse Functional pEC50 = 8.4 8.4 -4 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
118722939 116240 None 0 Mouse Functional pEC50 = 8.4 8.4 -6 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358547 116240 None 0 Mouse Functional pEC50 = 8.4 8.4 -6 4
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1334 1501 None 7 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
16133814 1501 None 7 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1501 None 7 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
133053557 163706 None 0 Human Functional pEC50 = 7.5 7.5 6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 163706 None 0 Human Functional pEC50 = 7.5 7.5 6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
155542040 173078 None 0 Mouse Functional pEC50 = 7.5 7.5 -151 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4519837 173078 None 0 Mouse Functional pEC50 = 7.5 7.5 -151 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
137633806 156481 None 0 Human Functional pEC50 = 7.5 7.5 -10 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 156481 None 0 Human Functional pEC50 = 7.5 7.5 -10 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
127047913 139924 None 0 Mouse Functional pEC50 = 7.5 7.5 -7 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799563 139924 None 0 Mouse Functional pEC50 = 7.5 7.5 -7 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL380638 212271 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
25128748 189991 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 189991 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
137656180 159028 None 0 Mouse Functional pEC50 = 6.5 6.5 -144 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4096678 159028 None 0 Mouse Functional pEC50 = 6.5 6.5 -144 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL413439 213070 None 0 Human Functional pEC50 = 6.5 6.5 -40 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44322924 107112 None 0 Human Functional pEC50 = 6.5 6.5 -42 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316038 107112 None 0 Human Functional pEC50 = 6.5 6.5 -42 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
137638218 156828 None 0 Mouse Functional pEC50 = 5.5 5.5 -66 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4071283 156828 None 0 Mouse Functional pEC50 = 5.5 5.5 -66 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
137657607 159636 None 0 Mouse Functional pEC50 = 5.5 5.5 -56 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4103567 159636 None 0 Mouse Functional pEC50 = 5.5 5.5 -56 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
155547842 173696 None 0 Mouse Functional pEC50 = 5.5 5.5 -125 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4535510 173696 None 0 Mouse Functional pEC50 = 5.5 5.5 -125 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 741 17 10 7 -1.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL3287060 211299 None 0 Mouse Functional pEC50 = 5.5 5.5 -52 5
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 assayAgonist 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
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
155554827 174619 None 0 Mouse Functional pEC50 = 4.5 4.5 -8 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4557656 174619 None 0 Mouse Functional pEC50 = 4.5 4.5 -8 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 621 16 8 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
45487410 197438 None 0 Mouse Functional pEC50 = 4.5 4.5 -97 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569696 197438 None 0 Mouse Functional pEC50 = 4.5 4.5 -97 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44394659 66954 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL186687 66954 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885712 8071 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 8071 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1204061 8071 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
44457021 97901 None 0 Mouse Functional pEC50 = 4.5 4.5 -17 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL272439 97901 None 0 Mouse Functional pEC50 = 4.5 4.5 -17 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 399 6 4 3 2.2 N=C(N)NCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL185869 209053 None 0 Human Functional pEC50 = 5.5 5.5 -89 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CCOC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL2369485 209628 None 0 Mouse Functional pEC50 = 6.5 6.5 -5 4
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)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](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
137641398 158316 None 0 Human Functional pEC50 = 6.5 6.5 -416 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 158316 None 0 Human Functional pEC50 = 6.5 6.5 -416 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 7.5 7.5 -35 8
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None CC(=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(N)=O 10.1021/acs.jmedchem.0c02041
CHEMBL411378 212881 None 0 Rat Functional pEC50 = 7.5 7.5 -56 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1 10.1021/jm030452x
164623182 185619 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 607 11 4 4 5.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4864094 185619 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 607 11 4 4 5.4 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44413938 138939 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 138939 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44394691 122903 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL360598 122903 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145988867 167103 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4289983 167103 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44413831 78064 None 0 Human Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL210008 78064 None 0 Human Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
134466953 156658 None 0 Mouse Functional pEC50 = 7.5 7.5 -91 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4069451 156658 None 0 Mouse Functional pEC50 = 7.5 7.5 -91 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
24882615 97492 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL270270 97492 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
51351024 58802 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318435 58802 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932358 58802 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688106 58802 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
102096778 58806 None 0 Mouse Functional pEC50 = 6.5 6.5 -35 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
51351277 58806 None 0 Mouse Functional pEC50 = 6.5 6.5 -35 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
53322400 58806 None 0 Mouse Functional pEC50 = 6.5 6.5 -35 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
91932360 58806 None 0 Mouse Functional pEC50 = 6.5 6.5 -35 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL1688111 58806 None 0 Mouse Functional pEC50 = 6.5 6.5 -35 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
122184910 122555 None 0 Human Functional pEC50 = 6.5 6.5 -30 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122555 None 0 Human Functional pEC50 = 6.5 6.5 -30 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 163834 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 163834 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 55 Human Functional pEC50 = 7.5 7.5 -58 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
92432 2688 None 55 Human Functional pEC50 = 7.5 7.5 -58 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL430239 2688 None 55 Human Functional pEC50 = 7.5 7.5 -58 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
44577519 188769 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL505536 188769 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
45487409 196897 None 0 Mouse Functional pEC50 = 4.5 4.5 -51 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566162 196897 None 0 Mouse Functional pEC50 = 4.5 4.5 -51 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44394783 126373 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365044 126373 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
16157270 212553 None 14 Mouse Functional pEC50 = 7.5 7.5 -22 7
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/acs.jmedchem.5b01894
CHEMBL405282 212553 None 14 Mouse Functional pEC50 = 7.5 7.5 -22 7
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/acs.jmedchem.5b01894
44413879 138902 None 0 Human Functional pEC50 = 6.5 6.5 -112 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 138902 None 0 Human Functional pEC50 = 6.5 6.5 -112 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL105113 208466 None 0 Mouse Functional pEC50 = 4.5 4.5 -30 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
90643802 111742 None 0 Mouse Functional pEC50 = 7.5 7.5 -41 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111742 None 0 Mouse Functional pEC50 = 7.5 7.5 -41 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
155547310 173611 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 750 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4533593 173611 None 0 Mouse Functional pEC50 = 6.5 6.5 -6 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 750 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
164621263 185482 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 11 3 3 7.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4862172 185482 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 11 3 3 7.2 CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL89270 215899 None 0 Human Functional pEC50 = 6.5 6.5 -11 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1016/s0960-894x(03)00552-3
11753695 8393 None 7 Human Functional pEC50 = 6.5 6.5 -281 8
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8393 None 7 Human Functional pEC50 = 6.5 6.5 -281 8
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
162670795 182826 None 0 Mouse Functional pEC50 = 7.4 7.4 -21 3
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 assayAgonist 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
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4791112 182826 None 0 Mouse Functional pEC50 = 7.4 7.4 -21 3
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 assayAgonist 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
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL410168 212804 None 0 Human Functional pEC50 = 7.4 7.4 -4 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
164624627 185879 None 0 Mouse Functional pEC50 = 6.4 6.4 -2 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868223 185879 None 0 Mouse Functional pEC50 = 6.4 6.4 -2 4
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 589 10 4 4 4.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
164627764 186564 None 0 Mouse Functional pEC50 = 6.4 6.4 2 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 603 11 4 4 4.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4878201 186564 None 0 Mouse Functional pEC50 = 6.4 6.4 2 2
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 603 11 4 4 4.8 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
46885523 7803 None 0 Human Functional pEC50 = 5.4 5.4 -512 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
CHEMBL1089461 7803 None 0 Human Functional pEC50 = 5.4 5.4 -512 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
46885711 8070 None 0 Human Functional pEC50 = 5.4 5.4 -123 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 8070 None 0 Human Functional pEC50 = 5.4 5.4 -123 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL446185 213944 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)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)NC1=O 10.1021/jm0510326
44415912 139226 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 139226 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44408287 75386 None 0 Human Functional pEC50 = 6.4 6.4 -218 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75386 None 0 Human Functional pEC50 = 6.4 6.4 -218 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL2371962 210159 None 0 Human Functional pEC50 = 6.4 6.4 -1412 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
164609130 184427 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 595 10 4 4 5.1 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4846261 184427 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 595 10 4 4 5.1 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
164615813 185144 None 0 Mouse Functional pEC50 = 5.4 5.4 -12 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 10 3 3 6.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4856877 185144 None 0 Mouse Functional pEC50 = 5.4 5.4 -12 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 594 10 3 3 6.4 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
11845804 79558 None 0 Human Functional pEC50 = 5.4 5.4 -467 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL211419 79558 None 0 Human Functional pEC50 = 5.4 5.4 -467 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 7.4 7.4 -35 8
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CC(=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(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL5094215 215481 None 0 Human Functional pEC50 = 7.4 7.4 -46 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
168285904 191670 None 0 Human Functional pEC50 = 6.4 6.4 -234 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 191670 None 0 Human Functional pEC50 = 6.4 6.4 -234 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
162654633 180644 None 0 Mouse Functional pEC50 = 7.4 7.4 -43 3
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 assayAgonist 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
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4754987 180644 None 0 Mouse Functional pEC50 = 7.4 7.4 -43 3
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 assayAgonist 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
ChEMBL 734 16 8 7 1.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL263878 210598 None 0 Human Functional pEC50 = 7.4 7.4 2 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
168290510 191897 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 191897 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5085972 215003 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL91957 215905 None 0 Human Functional pEC50 = 6.4 6.4 -35 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
137659091 159340 None 0 Mouse Functional pEC50 = 5.4 5.4 -41 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4100160 159340 None 0 Mouse Functional pEC50 = 5.4 5.4 -41 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
51350673 58800 None 0 Mouse Functional pEC50 = 5.4 5.4 -20 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53317148 58800 None 0 Mouse Functional pEC50 = 5.4 5.4 -20 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932362 58800 None 0 Mouse Functional pEC50 = 5.4 5.4 -20 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688104 58800 None 0 Mouse Functional pEC50 = 5.4 5.4 -20 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
122184909 122554 None 0 Human Functional pEC50 = 5.4 5.4 -13 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122554 None 0 Human Functional pEC50 = 5.4 5.4 -13 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077811 214516 None 0 Human Functional pEC50 = 6.4 6.4 -72 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
155553683 174183 None 0 Mouse Functional pEC50 = 8.4 8.4 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4547556 174183 None 0 Mouse Functional pEC50 = 8.4 8.4 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL5080489 214689 None 0 Human Functional pEC50 = 8.4 8.4 -4 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
145976863 163758 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163758 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1324 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
1324 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 25 Human Functional pEC50 = 8.4 8.4 -15 9
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
CHEMBL439128 213825 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
44394623 141538 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL384720 141538 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322896 167972 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 167972 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25133210 169457 None 0 Human Functional pEC50 = 7.4 7.4 -44 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 169457 None 0 Human Functional pEC50 = 7.4 7.4 -44 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
134463477 159252 None 0 Mouse Functional pEC50 = 7.4 7.4 -131 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4099127 159252 None 0 Mouse Functional pEC50 = 7.4 7.4 -131 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
132180597 156171 None 0 Mouse Functional pEC50 = 7.4 7.4 -275 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4063911 156171 None 0 Mouse Functional pEC50 = 7.4 7.4 -275 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
155550083 173914 None 0 Mouse Functional pEC50 = 7.4 7.4 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4540411 173914 None 0 Mouse Functional pEC50 = 7.4 7.4 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155556466 174416 None 0 Mouse Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4552764 174416 None 0 Mouse Functional pEC50 = 7.4 7.4 -56 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
162666503 182230 None 0 Mouse Functional pEC50 = 7.4 7.4 -36 3
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 assayAgonist 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
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4783292 182230 None 0 Mouse Functional pEC50 = 7.4 7.4 -36 3
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 assayAgonist 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
ChEMBL 696 15 7 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
44322787 105964 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 105964 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162669632 182565 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182565 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL409049 212745 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
137646802 157951 None 0 Mouse Functional pEC50 = 5.4 5.4 -19 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084671 157951 None 0 Mouse Functional pEC50 = 5.4 5.4 -19 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 888 18 8 7 3.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
155531140 171618 None 0 Mouse Functional pEC50 = 5.4 5.4 -13 4
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 assayAgonist 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
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4465466 171618 None 0 Mouse Functional pEC50 = 5.4 5.4 -13 4
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 assayAgonist 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
ChEMBL 666 16 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
164621924 185951 None 0 Mouse Functional pEC50 = 5.4 5.4 -6 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 10 3 3 5.7 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4869531 185951 None 0 Mouse Functional pEC50 = 5.4 5.4 -6 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 587 10 3 3 5.7 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N 10.1021/acs.jmedchem.0c02041
44347927 157276 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 157276 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2323788 209514 None 0 Mouse Functional pEC50 = 5.4 5.4 -75 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
16007263 79796 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 79796 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394784 126295 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365019 126295 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL321870 211232 None 0 Mouse Functional pEC50 = 5.4 5.4 -79 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
46885526 7764 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
CHEMBL1089135 7764 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
CHEMBL1204056 7764 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
122179552 121487 None 0 Mouse Functional pEC50 = 6.4 6.4 -74 4
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
CHEMBL3582446 121487 None 0 Mouse Functional pEC50 = 6.4 6.4 -74 4
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
44456957 98038 None 0 Mouse Functional pEC50 = 5.4 5.4 -18 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 432 5 1 2 5.2 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21 10.1021/jm701303z
CHEMBL273044 98038 None 0 Mouse Functional pEC50 = 5.4 5.4 -18 3
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 432 5 1 2 5.2 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21 10.1021/jm701303z
44413931 78015 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 78015 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
145948876 167483 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 167483 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
164624386 186198 None 0 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 10 4 4 5.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4872932 186198 None 0 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 10 4 4 5.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44394693 96598 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263234 96598 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL382369 212305 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
164627732 186494 None 0 Mouse Functional pEC50 = 5.4 5.4 -14 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 10 3 3 7.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4877232 186494 None 0 Mouse Functional pEC50 = 5.4 5.4 -14 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 598 10 3 3 7.0 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
44441647 154690 None 0 Human Functional pEC50 = 6.4 6.4 -18 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399714 154690 None 0 Human Functional pEC50 = 6.4 6.4 -18 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
168278924 191066 None 0 Human Functional pEC50 = 6.4 6.4 -22 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 191066 None 0 Human Functional pEC50 = 6.4 6.4 -22 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL50056 214119 None 2 Mouse Functional pEC50 = 5.4 5.4 -138 7
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL50056 214119 None 2 Mouse Functional pEC50 = 5.4 5.4 -138 7
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
45487404 197436 None 0 Mouse Functional pEC50 = 4.4 4.4 -8709 5
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569694 197436 None 0 Mouse Functional pEC50 = 4.4 4.4 -8709 5
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44569176 172545 None 0 Human Functional pEC50 = 7.4 7.4 -48 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 172545 None 0 Human Functional pEC50 = 7.4 7.4 -48 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
25129107 173777 None 0 Human Functional pEC50 = 7.4 7.4 -36 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 173777 None 0 Human Functional pEC50 = 7.4 7.4 -36 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
11181928 166157 None 0 Mouse Functional pEC50 = 7.4 7.4 -13 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL426282 166157 None 0 Mouse Functional pEC50 = 7.4 7.4 -13 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
155561730 175653 None 0 Mouse Functional pEC50 = 5.4 5.4 -144 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4581269 175653 None 0 Mouse Functional pEC50 = 5.4 5.4 -144 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 684 14 7 6 -0.3 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44305956 102761 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL305132 102761 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 4
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
44305784 203339 None 0 Mouse Functional pEC50 = 5.4 5.4 1 3
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 447 8 4 3 3.4 CC1CCN(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL64967 203339 None 0 Mouse Functional pEC50 = 5.4 5.4 1 3
Agonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cellsAgonist activity on mouse Melanocortin 3 receptor (mMC3R) stably expressed in HEK cells
ChEMBL 447 8 4 3 3.4 CC1CCN(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
155550338 174308 None 0 Mouse Functional pEC50 = 4.4 4.4 -630 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 649 17 10 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550246 174308 None 0 Mouse Functional pEC50 = 4.4 4.4 -630 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 649 17 10 7 -1.6 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL317228 211200 None 0 Mouse Functional pEC50 = 4.4 4.4 -10 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)c1ccccc1 10.1021/jm010524p
CHEMBL184870 209051 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None C=CCNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322959 156075 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 156075 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408154 141362 None 0 Human Functional pEC50 = 6.4 6.4 -316 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 141362 None 0 Human Functional pEC50 = 6.4 6.4 -316 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
44322788 157383 None 0 Human Functional pEC50 = 6.4 6.4 -58 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 157383 None 0 Human Functional pEC50 = 6.4 6.4 -58 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2323789 209515 None 0 Mouse Functional pEC50 = 5.4 5.4 -2290 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44394690 124648 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL364119 124648 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168285101 191644 None 0 Human Functional pEC50 = 6.3 6.3 -213 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191644 None 0 Human Functional pEC50 = 6.3 6.3 -213 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
46885760 8278 None 0 Human Functional pEC50 = 5.3 5.3 -102 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
CHEMBL1092550 8278 None 0 Human Functional pEC50 = 5.3 5.3 -102 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
137653916 158580 None 0 Mouse Functional pEC50 = 6.3 6.3 -18 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4091894 158580 None 0 Mouse Functional pEC50 = 6.3 6.3 -18 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
44394582 168374 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434544 168374 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
102096778 58806 None 0 Mouse Functional pEC50 = 5.3 5.3 -35 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
51351277 58806 None 0 Mouse Functional pEC50 = 5.3 5.3 -35 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322400 58806 None 0 Mouse Functional pEC50 = 5.3 5.3 -35 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932360 58806 None 0 Mouse Functional pEC50 = 5.3 5.3 -35 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688111 58806 None 0 Mouse Functional pEC50 = 5.3 5.3 -35 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL3600840 211817 None 0 Human Functional pEC50 = 6.3 6.3 -1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
137641157 157064 None 0 Human Functional pEC50 = 6.3 6.3 -131 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 157064 None 0 Human Functional pEC50 = 6.3 6.3 -131 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
90643804 111744 None 0 Mouse Functional pEC50 = 7.3 7.3 -42 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111744 None 0 Mouse Functional pEC50 = 7.3 7.3 -42 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
127046235 139638 None 0 Mouse Functional pEC50 = 7.3 7.3 -380 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3797690 139638 None 0 Mouse Functional pEC50 = 7.3 7.3 -380 5
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
44394581 122149 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359702 122149 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL2323795 209521 None 0 Mouse Functional pEC50 = 7.3 7.3 -97 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
46885482 8330 None 0 Human Functional pEC50 = 6.3 6.3 -81 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092860 8330 None 0 Human Functional pEC50 = 6.3 6.3 -81 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
51351151 58805 None 0 Mouse Functional pEC50 = 6.3 6.3 -15 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318437 58805 None 0 Mouse Functional pEC50 = 6.3 6.3 -15 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932359 58805 None 0 Mouse Functional pEC50 = 6.3 6.3 -15 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688110 58805 None 0 Mouse Functional pEC50 = 6.3 6.3 -15 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
44394580 122148 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359701 122148 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145972289 164520 None 0 Human Functional pEC50 = 8.3 8.3 27 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 164520 None 0 Human Functional pEC50 = 8.3 8.3 27 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
92432 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
137637283 155980 None 0 Human Functional pEC50 = 8.3 8.3 -15 3
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 155980 None 0 Human Functional pEC50 = 8.3 8.3 -15 3
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
1323 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
1323 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 55 Human Functional pEC50 = 8.3 8.3 -58 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
11158573 71119 None 0 Mouse Functional pEC50 = 8.3 8.3 -12 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL195439 71119 None 0 Mouse Functional pEC50 = 8.3 8.3 -12 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL405791 212580 None 0 Rat Functional pEC50 = 8.3 8.3 -1 4
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ncc[nH]2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL2372570 210271 None 0 Human Functional pEC50 = 8.3 8.3 -53 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
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](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O 10.1021/jm9017866
44415920 80371 None 0 Human Functional pEC50 = 8.3 8.3 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 80371 None 0 Human Functional pEC50 = 8.3 8.3 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
1334 1501 None 7 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 7 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 7 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
44577515 189007 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 189007 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
155555182 174321 None 0 Mouse Functional pEC50 = 7.3 7.3 -20 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 778 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550582 174321 None 0 Mouse Functional pEC50 = 7.3 7.3 -20 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 778 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155561743 175772 None 0 Mouse Functional pEC50 = 7.3 7.3 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4583714 175772 None 0 Mouse Functional pEC50 = 7.3 7.3 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155568641 176097 None 0 Mouse Functional pEC50 = 7.3 7.3 -83 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4591394 176097 None 0 Mouse Functional pEC50 = 7.3 7.3 -83 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
46885415 8279 None 0 Human Functional pEC50 = 6.3 6.3 -15 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092571 8279 None 0 Human Functional pEC50 = 6.3 6.3 -15 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
155566298 175793 None 0 Mouse Functional pEC50 = 6.3 6.3 -38 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4584189 175793 None 0 Mouse Functional pEC50 = 6.3 6.3 -38 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137634306 156322 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4065669 156322 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
155554244 174949 None 0 Mouse Functional pEC50 = 4.3 4.3 -28 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4565607 174949 None 0 Mouse Functional pEC50 = 4.3 4.3 -28 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 630 15 8 7 -0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
168277543 190675 None 0 Human Functional pEC50 = 6.3 6.3 -125 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 190675 None 0 Human Functional pEC50 = 6.3 6.3 -125 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
25129109 188702 None 0 Human Functional pEC50 = 7.3 7.3 -30 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 188702 None 0 Human Functional pEC50 = 7.3 7.3 -30 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
132180653 175059 None 0 Mouse Functional pEC50 = 7.3 7.3 -51 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567961 175059 None 0 Mouse Functional pEC50 = 7.3 7.3 -51 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
137648053 157539 None 0 Mouse Functional pEC50 = 6.3 6.3 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4080169 157539 None 0 Mouse Functional pEC50 = 6.3 6.3 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
122184911 122556 None 0 Human Functional pEC50 = 5.3 5.3 -10 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122556 None 0 Human Functional pEC50 = 5.3 5.3 -10 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
118735099 118799 None 0 Human Functional pEC50 = 7.3 7.3 -4 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 118799 None 0 Human Functional pEC50 = 7.3 7.3 -4 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
25133209 173351 None 0 Human Functional pEC50 = 7.3 7.3 -19 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 173351 None 0 Human Functional pEC50 = 7.3 7.3 -19 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
1334 1501 None 7 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 7 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 7 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
164621414 185774 None 0 Mouse Functional pEC50 = 5.3 5.3 -7 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4866532 185774 None 0 Mouse Functional pEC50 = 5.3 5.3 -7 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 531 12 4 4 4.4 CC(C)CCCN1C(=N)N([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL503449 214166 None 0 Mouse Functional pEC50 = 6.3 6.3 -99 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL444219 213930 None 0 Mouse Functional pEC50 = 7.3 7.3 -120 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
137636965 156216 None 0 Human Functional pEC50 = 5.3 5.3 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 156216 None 0 Human Functional pEC50 = 5.3 5.3 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44408173 75401 None 0 Human Functional pEC50 = 6.3 6.3 -186 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75401 None 0 Human Functional pEC50 = 6.3 6.3 -186 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
137658359 159571 None 0 Mouse Functional pEC50 = 6.3 6.3 -33 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102774 159571 None 0 Mouse Functional pEC50 = 6.3 6.3 -33 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
44413876 79744 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 79744 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 79744 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 79744 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
25132526 188923 None 0 Human Functional pEC50 = 6.3 6.3 -69 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
CHEMBL507876 188923 None 0 Human Functional pEC50 = 6.3 6.3 -69 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
118735103 118803 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118803 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
90643806 111746 None 0 Mouse Functional pEC50 = 7.3 7.3 -87 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111746 None 0 Mouse Functional pEC50 = 7.3 7.3 -87 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 7.3 7.3 -35 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CC(=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(N)=O 10.1021/acs.jmedchem.5b01894
44408253 140344 None 0 Human Functional pEC50 = 6.3 6.3 -54 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 140344 None 0 Human Functional pEC50 = 6.3 6.3 -54 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL2304248 209485 None 0 Mouse Functional pEC50 = 5.3 5.3 -3 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL183315 209043 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394734 64557 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181494 64557 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44577520 188824 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 188824 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL5078687 214580 None 0 Human Functional pEC50 = 7.3 7.3 -25 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44413913 138673 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 138673 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
145988152 167044 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 167044 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
132180599 156893 None 0 Mouse Functional pEC50 = 7.2 7.2 1 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4072129 156893 None 0 Mouse Functional pEC50 = 7.2 7.2 1 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
46885759 8276 None 0 Human Functional pEC50 = 6.2 6.2 -95 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092548 8276 None 0 Human Functional pEC50 = 6.2 6.2 -95 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
44322994 106997 None 0 Human Functional pEC50 = 6.2 6.2 -60 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315258 106997 None 0 Human Functional pEC50 = 6.2 6.2 -60 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25129108 172696 None 0 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL450236 172696 None 0 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
44322977 111569 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 111569 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
45487414 197281 None 0 Mouse Functional pEC50 = 4.2 4.2 -54 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568577 197281 None 0 Mouse Functional pEC50 = 4.2 4.2 -54 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 621 16 8 6 0.8 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
11061068 31292 None 0 Human Functional pEC50 = 7.2 7.2 -138 3
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 31292 None 0 Human Functional pEC50 = 7.2 7.2 -138 3
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL2372365 210224 None 0 Rat Functional pEC50 = 7.2 7.2 -1 3
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC(C)(C)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
44408155 140553 None 0 Human Functional pEC50 = 6.2 6.2 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140553 None 0 Human Functional pEC50 = 6.2 6.2 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44413932 137546 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 137546 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
44415918 141549 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 141549 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
155564058 175334 None 0 Mouse Functional pEC50 = 8.2 8.2 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4574056 175334 None 0 Mouse Functional pEC50 = 8.2 8.2 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44275650 94054 None 0 Human Functional pEC50 = 8.2 8.2 -15 4
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=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](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 94054 None 0 Human Functional pEC50 = 8.2 8.2 -15 4
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=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](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
44322895 163370 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 163370 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370964 209967 None 0 Human Functional pEC50 = 8.2 8.2 -47 4
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 209967 None 0 Human Functional pEC50 = 8.2 8.2 -47 4
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL5080784 214706 None 0 Human Functional pEC50 = 8.2 8.2 -9 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090285 215253 None 0 Human Functional pEC50 = 8.2 8.2 -8 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
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/jm049579s
16133793 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
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/jm049579s
44273719 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
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/jm049579s
CHEMBL214332 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
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/jm049579s
16132144 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
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/jm030111j
16133793 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
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/jm030111j
44273719 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
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/jm030111j
CHEMBL214332 209279 None 36 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
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/jm030111j
1324 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16154396 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727.0 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
44285019 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
57514683 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
91898441 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL441738 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
DB04931 302 None 25 Human Functional pEC50 = 8.2 8.2 -15 9
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL405335 212556 None 0 Mouse Functional pEC50 = 8.2 8.2 -39 4
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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/jm010061n
155539948 172886 None 0 Mouse Functional pEC50 = 7.2 7.2 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4515666 172886 None 0 Mouse Functional pEC50 = 7.2 7.2 -30 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155542149 173092 None 0 Mouse Functional pEC50 = 7.2 7.2 -30 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 740 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4520119 173092 None 0 Mouse Functional pEC50 = 7.2 7.2 -30 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 740 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
155563055 175295 None 0 Mouse Functional pEC50 = 7.2 7.2 -12 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4573041 175295 None 0 Mouse Functional pEC50 = 7.2 7.2 -12 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
162670951 182838 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182838 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
46885558 7809 None 0 Human Functional pEC50 = 6.2 6.2 -151 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089483 7809 None 0 Human Functional pEC50 = 6.2 6.2 -151 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
137649368 157406 None 0 Mouse Functional pEC50 = 6.2 6.2 -70 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4078495 157406 None 0 Mouse Functional pEC50 = 6.2 6.2 -70 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
9852256 175367 None 0 Mouse Functional pEC50 = 5.2 5.2 -15 4
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 assayAgonist 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
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4574756 175367 None 0 Mouse Functional pEC50 = 5.2 5.2 -15 4
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 assayAgonist 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
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
162670951 182838 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182838 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
137651071 157467 None 0 Mouse Functional pEC50 = 6.2 6.2 -158 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079298 157467 None 0 Mouse Functional pEC50 = 6.2 6.2 -158 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL451423 213968 None 0 Mouse Functional pEC50 = 6.2 6.2 -47 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL509582 215546 None 0 Human Functional pEC50 = 6.2 6.2 -16 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
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]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
164625186 185967 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
CHEMBL4869669 185967 None 0 Mouse Functional pEC50 = 5.2 5.2 -6 3
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 11 3 3 6.5 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1 10.1021/acs.jmedchem.0c02041
137637656 156238 None 0 Human Functional pEC50 = 6.2 6.2 -69 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 156238 None 0 Human Functional pEC50 = 6.2 6.2 -69 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL2448525 210499 None 0 Mouse Functional pEC50 = 4.2 4.2 -977 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL411400 212883 None 0 Rat Functional pEC50 = 7.2 7.2 -457 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=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](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O 10.1021/jm030452x
44408275 75419 None 0 Human Functional pEC50 = 6.2 6.2 -120 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75419 None 0 Human Functional pEC50 = 6.2 6.2 -120 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44323034 206530 None 0 Human Functional pEC50 = 6.2 6.2 -46 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 206530 None 0 Human Functional pEC50 = 6.2 6.2 -46 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394735 123315 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361578 123315 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168273822 190570 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 190570 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
46885481 7755 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089104 7755 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
162671821 182903 None 0 Mouse Functional pEC50 = 7.2 7.2 -4 3
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 assayAgonist 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
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL4792291 182903 None 0 Mouse Functional pEC50 = 7.2 7.2 -4 3
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 assayAgonist 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
ChEMBL 725 17 8 7 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acsmedchemlett.0c00561
CHEMBL415200 213179 None 0 Rat Functional pEC50 = 6.2 6.2 -77 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL184644 209050 None 0 Human Functional pEC50 = 5.2 5.2 -16 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394736 123316 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361579 123316 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11846844 140079 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 140079 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44441642 154405 None 0 Human Functional pEC50 = 6.2 6.2 -77 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 154405 None 0 Human Functional pEC50 = 6.2 6.2 -77 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137640703 157097 None 0 Human Functional pEC50 = 5.2 5.2 -1202 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 157097 None 0 Human Functional pEC50 = 5.2 5.2 -1202 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL264190 210608 None 1 Human Functional pEC50 = 8.2 8.2 -3 8
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None CC(=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(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL406842 212624 None 0 Rat Functional pEC50 = 8.1 8.1 -66 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL5077095 214479 None 0 Human Functional pEC50 = 8.1 8.1 -57 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
162665266 182181 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 3
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 assayAgonist 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
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
CHEMBL4782693 182181 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 3
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 assayAgonist 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
ChEMBL 668 14 5 6 1.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acsmedchemlett.0c00561
155549302 173803 None 0 Mouse Functional pEC50 = 6.2 6.2 -7 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4538209 173803 None 0 Mouse Functional pEC50 = 6.2 6.2 -7 3
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 626 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
1334 1501 None 7 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 7 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 7 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
10146211 64329 None 0 Human Functional pEC50 = 5.2 5.2 -2511 3
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 64329 None 0 Human Functional pEC50 = 5.2 5.2 -2511 3
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
122184577 122429 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 122429 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
46885480 7754 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 7754 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44322812 112382 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 112382 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2323800 209526 None 0 Mouse Functional pEC50 = 5.2 5.2 -446 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
46232226 201083 None 0 Mouse Functional pEC50 = 5.1 5.1 -891 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602853 201083 None 0 Mouse Functional pEC50 = 5.1 5.1 -891 4
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL5075506 214379 None 0 Human Functional pEC50 = 7.1 7.1 -512 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
155549865 173856 None 0 Mouse Functional pEC50 = 6.1 6.1 -18 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539175 173856 None 0 Mouse Functional pEC50 = 6.1 6.1 -18 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 658 17 7 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
137647009 157854 None 0 Human Functional pEC50 = 6.1 6.1 -30 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4083755 157854 None 0 Human Functional pEC50 = 6.1 6.1 -30 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
145964837 164347 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[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/acs.jmedchem.8b00488
CHEMBL4212629 164347 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[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/acs.jmedchem.8b00488
CHEMBL264190 210608 None 1 Mouse Functional pEC50 = 7.1 7.1 -35 8
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None CC(=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(N)=O 10.1021/acs.jmedchem.7b00301
45487413 197251 None 0 Mouse Functional pEC50 = 5.1 5.1 -6 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568409 197251 None 0 Mouse Functional pEC50 = 5.1 5.1 -6 4
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
137646617 157544 None 0 Human Functional pEC50 = 5.1 5.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 157544 None 0 Human Functional pEC50 = 5.1 5.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46885524 7804 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1089462 7804 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1204054 7804 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
1324 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16154396 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16197727 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16197727.0 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
44285019 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
57514683 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
91898441 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
CHEMBL441738 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
DB04931 302 None 25 Mouse Functional pEC50 = 7.1 7.1 -6 9
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cellsCompound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
CHEMBL406891 212626 None 0 Rat Functional pEC50 = 7.1 7.1 -34 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL3349030 211405 None 0 Human Functional pEC50 = 6.1 6.1 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL3600922 211825 None 0 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44394730 132487 None 0 Human Functional pEC50 = 6.1 6.1 -53 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL369770 132487 None 0 Human Functional pEC50 = 6.1 6.1 -53 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137647538 157962 None 0 Human Functional pEC50 = 6.1 6.1 -1445 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 157962 None 0 Human Functional pEC50 = 6.1 6.1 -1445 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145975465 163949 None 0 Human Functional pEC50 = 7.1 7.1 -6 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 163949 None 0 Human Functional pEC50 = 7.1 7.1 -6 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145964017 164041 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 164041 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
53318436 58803 None 0 Mouse Functional pEC50 = 5.1 5.1 -46 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
CHEMBL1688108 58803 None 0 Mouse Functional pEC50 = 5.1 5.1 -46 4
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 814 17 10 9 -0.4 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101425m
46919520 15138 None 0 Human Functional pEC50 = 6.1 6.1 -549 6
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15138 None 0 Human Functional pEC50 = 6.1 6.1 -549 6
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
162643435 181667 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181667 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 181667 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181667 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
122184912 122558 None 0 Human Functional pEC50 = 6.1 6.1 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122558 None 0 Human Functional pEC50 = 6.1 6.1 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
15602927 157882 None 0 Mouse Functional pEC50 = 6.1 6.1 -194 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL408398 157882 None 0 Mouse Functional pEC50 = 6.1 6.1 -194 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL455826 214009 None 0 Mouse Functional pEC50 = 6.1 6.1 -15 4
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL2323792 209518 None 0 Mouse Functional pEC50 = 5.1 5.1 1 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44457067 97742 None 0 Mouse Functional pEC50 = 5.1 5.1 -1548 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL271586 97742 None 0 Mouse Functional pEC50 = 5.1 5.1 -1548 5
Agonist activity at mouse MC3R expressed in HEK293 cellsAgonist activity at mouse MC3R expressed in HEK293 cells
ChEMBL 877 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
44335147 4592 None 0 Mouse Functional pEC50 = 5.1 5.1 -12 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 4592 None 0 Mouse Functional pEC50 = 5.1 5.1 -12 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
49862377 15041 None 0 Human Functional pEC50 = 7.1 7.1 -13 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 15041 None 0 Human Functional pEC50 = 7.1 7.1 -13 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
155543031 173181 None 0 Mouse Functional pEC50 = 8.1 8.1 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4522298 173181 None 0 Mouse Functional pEC50 = 8.1 8.1 -13 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155560756 175085 None 0 Mouse Functional pEC50 = 6.1 6.1 -15 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4568647 175085 None 0 Mouse Functional pEC50 = 6.1 6.1 -15 4
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 756 14 6 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL3600921 211824 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2323797 209523 None 0 Mouse Functional pEC50 = 5.1 5.1 -426 4
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm301253y
137648144 157758 None 0 Human Functional pEC50 = 6.1 6.1 -38 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4082585 157758 None 0 Human Functional pEC50 = 6.1 6.1 -38 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
11845438 137623 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL375775 137623 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44394627 124081 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363272 124081 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44416135 80184 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 80184 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
25133208 171994 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 171994 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL491870 214077 None 0 Mouse Functional pEC50 = 7.1 7.1 -213 5
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
44441646 154088 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 154088 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL88185 215896 None 0 Human Functional pEC50 = 6.1 6.1 -38 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25133207 172943 None 0 Human Functional pEC50 = 6.1 6.1 -18 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
CHEMBL451694 172943 None 0 Human Functional pEC50 = 6.1 6.1 -18 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
44413930 138648 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 138648 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
122179551 121486 None 0 Mouse Functional pEC50 = 6.1 6.1 -22 4
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
CHEMBL3582445 121486 None 0 Mouse Functional pEC50 = 6.1 6.1 -22 4
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
44394787 165988 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL425348 165988 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181161 208980 None 0 Human Functional pEC50 = 7.1 7.1 -10 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394585 66766 None 0 Human Functional pEC50 = 6.1 6.1 -63 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL185868 66766 None 0 Human Functional pEC50 = 6.1 6.1 -63 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137636677 156100 None 0 Human Functional pEC50 = 5.1 5.1 -295 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 156100 None 0 Human Functional pEC50 = 5.1 5.1 -295 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11845813 139804 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 139804 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL410217 212808 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)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)NC1=O 10.1021/jm960845e
44408252 140669 None 0 Human Functional pEC50 = 6.1 6.1 -77 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140669 None 0 Human Functional pEC50 = 6.1 6.1 -77 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862378 15042 None 0 Human Functional pEC50 = 6.1 6.1 -83 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 15042 None 0 Human Functional pEC50 = 6.1 6.1 -83 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
44394584 96570 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263047 96570 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137636060 156231 None 0 Mouse Functional pEC50 = 5.1 5.1 2 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4064728 156231 None 0 Mouse Functional pEC50 = 5.1 5.1 2 2
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 850 15 7 7 2.5 CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
10078903 68019 None 0 Mouse Functional pEC50 = 8.0 8.0 -28 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191303 68019 None 0 Mouse Functional pEC50 = 8.0 8.0 -28 4
In vitro agonist potency for Mouse Melanocortin 3 receptorIn vitro agonist potency for Mouse Melanocortin 3 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44323029 207181 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 207181 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285801 191481 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 191481 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600841 211818 None 0 Human Functional pEC50 = 8 8.0 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
49862375 15039 None 0 Human Functional pEC50 = 7.1 7.1 -16 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 15039 None 0 Human Functional pEC50 = 7.1 7.1 -16 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
163196518 192129 None 2 Human Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 192129 None 2 Human Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL187125 209055 None 0 Human Functional pEC50 = 6.0 6.0 -30 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)Nc1ccco1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448631 95070 None 0 Human Functional pEC50 = 6.0 6.0 -416 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95070 None 0 Human Functional pEC50 = 6.0 6.0 -416 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL359765 211807 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL343094 211697 None 0 Mouse Functional pEC50 = 5.0 5.0 -57 4
Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
44322987 96732 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 96732 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
137653704 158633 None 0 Mouse Functional pEC50 = 6.0 6.0 -6 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4092424 158633 None 0 Mouse Functional pEC50 = 6.0 6.0 -6 4
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
90643808 111747 None 0 Mouse Functional pEC50 = 7.0 7.0 -93 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111747 None 0 Mouse Functional pEC50 = 7.0 7.0 -93 5
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
24774356 94825 None 0 Human Functional pEC50 = 7.0 7.0 8 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253574 94825 None 0 Human Functional pEC50 = 7.0 7.0 8 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL5091245 215300 None 0 Human Functional pEC50 = 7.0 7.0 -26 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL414778 213156 None 0 Human Functional pEC50 = 6.0 6.0 -154 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL50056 214119 None 2 Mouse Functional pEC50 = 6.0 6.0 -138 7
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
44394586 126779 None 0 Human Functional pEC50 = 6.0 6.0 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365385 126779 None 0 Human Functional pEC50 = 6.0 6.0 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448629 167463 None 0 Human Functional pEC50 = 7.0 7.0 -346 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167463 None 0 Human Functional pEC50 = 7.0 7.0 -346 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2112008 209226 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44323033 107152 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 107152 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132867 172498 None 0 Human Functional pEC50 = 6.0 6.0 -38 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 172498 None 0 Human Functional pEC50 = 6.0 6.0 -38 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44408276 75507 None 0 Human Functional pEC50 = 6 6.0 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75507 None 0 Human Functional pEC50 = 6 6.0 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
6918813 131371 None 3 Human Functional pEC50 = 6 6.0 -144 4
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131371 None 3 Human Functional pEC50 = 6 6.0 -144 4
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44335147 4592 None 0 Mouse Functional pEC50 = 5 5.0 -12 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 4592 None 0 Mouse Functional pEC50 = 5 5.0 -12 4
Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
44394692 66214 None 0 Human Functional pEC50 = 6 6.0 -33 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184466 66214 None 0 Human Functional pEC50 = 6 6.0 -33 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11753695 8393 None 7 Rat Functional pEC50 = 6 6.0 -501 8
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8393 None 7 Rat Functional pEC50 = 6 6.0 -501 8
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL2370968 209971 None 0 Human Functional pIC50 = 8.0 8.0 -63 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370968 209971 None 0 Human Functional pIC50 = 8.0 8.0 -63 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 209967 None 0 Human Functional pIC50 = 8.0 8.0 -47 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 209967 None 0 Human Functional pIC50 = 8.0 8.0 -47 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
162673640 182982 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 182982 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 182982 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 182982 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677173 183528 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 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](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 183528 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 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](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677173 183528 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 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](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 183528 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 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](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162664942 182193 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 182193 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162644475 181805 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 181805 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162644475 181805 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 181805 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
101043845 190392 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 190392 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
101043845 190392 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 190392 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
162668987 182590 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182590 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 182590 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182590 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 183314 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 183314 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 183314 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 183314 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162665567 182349 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 182349 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162665567 182349 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 182349 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 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]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162672763 183124 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183124 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183124 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183124 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162667953 182537 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 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]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 182537 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 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]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
162667953 182537 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 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]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 182537 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 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]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
162675203 183261 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 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](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 183261 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 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](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675203 183261 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 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](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 183261 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 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](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
10855168 181906 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 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]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 181906 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 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]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
10855168 181906 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 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]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 181906 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 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]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
162673931 183058 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183058 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 183058 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183058 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
101176453 182962 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 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]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 182962 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 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]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
101176453 182962 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 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]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 182962 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 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]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
162643518 181711 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181711 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 181711 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181711 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 183460 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 183460 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 183460 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 183460 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183021 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183021 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183021 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183021 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183453 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183453 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183557 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183557 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183557 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183557 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183453 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183453 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181724 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181724 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181724 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181724 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183053 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183053 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183053 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183053 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1325 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
1325 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 14 Human Functional pIC50 = 7.1 7.1 -125 5
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
162664942 182193 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 182193 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL253364 210509 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](N)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2323796 209522 None 0 Mouse Functional pKd = 9.9 9.9 - 3
Antagonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAntagonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44445083 154305 None 0 Human Functional pKd = 9.8 9.8 2 3
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 154305 None 0 Human Functional pKd = 9.8 9.8 2 3
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
122184576 122428 None 0 Human Functional pKd = 9.1 9.1 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 122428 None 0 Human Functional pKd = 9.1 9.1 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
164619641 185726 None 0 Mouse Functional pKd = 9 9.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4865888 185726 None 0 Mouse Functional pKd = 9 9.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL266288 96963 None 0 Mouse Functional pKd = 8.9 8.9 - 1
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 5507 70 67 87 -15.6 CSCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CSSSSC[C@@H]3NC(=O)[C@@H]4CCCN4C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](CSSSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(N)=O)NC1=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CSSSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N4)NC3=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSSSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCN=C(N)N)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/jm0303608
164613340 184720 None 0 Mouse Functional pKd = 8.8 8.8 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4850510 184720 None 0 Mouse Functional pKd = 8.8 8.8 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
127035019 136436 None 0 Mouse Functional pKd = 8.8 8.8 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735607 136436 None 0 Mouse Functional pKd = 8.8 8.8 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL2096742 209206 None 0 Human Functional pKd = 8.7 8.7 -3 6
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
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/jm070461w
164612217 184845 None 0 Mouse Functional pKd = 8.7 8.7 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852297 184845 None 0 Mouse Functional pKd = 8.7 8.7 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
122184635 122434 None 0 Human Functional pKd = 8 8.0 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122434 None 0 Human Functional pKd = 8 8.0 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145951083 162976 None 0 Mouse Functional pKd = 8 8.0 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1033 15 12 10 -0.4 C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4175108 162976 None 0 Mouse Functional pKd = 8 8.0 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1033 15 12 10 -0.4 C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
164620129 185747 None 0 Mouse Functional pKd = 8 8.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866219 185747 None 0 Mouse Functional pKd = 8 8.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613340 184720 None 0 Mouse Functional pKd = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4850510 184720 None 0 Mouse Functional pKd = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164626062 186600 None 0 Mouse Functional pKd = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4878799 186600 None 0 Mouse Functional pKd = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
162645080 179450 None 0 Mouse Functional pKd = 6 6.0 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4740561 179450 None 0 Mouse Functional pKd = 6 6.0 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
164619091 186186 None 0 Mouse Functional pKd = 6 6.0 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872732 186186 None 0 Mouse Functional pKd = 6 6.0 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164625782 186481 None 0 Mouse Functional pKd = 6 6.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4876953 186481 None 0 Mouse Functional pKd = 6 6.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
145957551 162264 None 0 Mouse Functional pKd = 7.9 7.9 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1015 17 13 11 -1.5 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4163787 162264 None 0 Mouse Functional pKd = 7.9 7.9 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1015 17 13 11 -1.5 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
162649541 180055 None 0 Mouse Functional pKd = 6.9 6.9 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 963 12 9 10 -0.8 C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4747778 180055 None 0 Mouse Functional pKd = 6.9 6.9 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 963 12 9 10 -0.8 C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
162662360 181471 None 0 Mouse Functional pKd = 6.9 6.9 - 2
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4764556 181471 None 0 Mouse Functional pKd = 6.9 6.9 - 2
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
164612091 184599 None 0 Mouse Functional pKd = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848905 184599 None 0 Mouse Functional pKd = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613676 185449 None 0 Mouse Functional pKd = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4861645 185449 None 0 Mouse Functional pKd = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
162676380 183366 None 0 Mouse Functional pKd = 5.9 5.9 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(CCCNC(=N)N)C(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4797774 183366 None 0 Mouse Functional pKd = 5.9 5.9 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(CCCNC(=N)N)C(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
137659851 159437 None 0 Mouse Functional pKd = 5.9 5.9 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 949 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4101128 159437 None 0 Mouse Functional pKd = 5.9 5.9 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 949 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
155548853 173809 None 0 Mouse Functional pKd = 5.9 5.9 -1380 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 173809 None 0 Mouse Functional pKd = 5.9 5.9 -1380 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
164619641 185726 None 0 Mouse Functional pKd = 7.8 7.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4865888 185726 None 0 Mouse Functional pKd = 7.8 7.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164618743 185590 None 0 Mouse Functional pKd = 7.8 7.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863637 185590 None 0 Mouse Functional pKd = 7.8 7.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
145950765 162833 None 0 Mouse Functional pKd = 6.8 6.8 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 964 12 11 11 -2.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4172753 162833 None 0 Mouse Functional pKd = 6.8 6.8 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 964 12 11 11 -2.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
164624484 185586 None 0 Mouse Functional pKd = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863587 185586 None 0 Mouse Functional pKd = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164620129 185747 None 0 Mouse Functional pKd = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866219 185747 None 0 Mouse Functional pKd = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL2373991 210381 None 0 Mouse Functional pKd = 6.8 6.8 -14 3
Antagonistic activity against mouse Melanocortin 3 ReceptorAntagonistic activity against mouse Melanocortin 3 Receptor
ChEMBL None None None CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/jm049620r
162667883 182414 None 0 Mouse Functional pKd = 5.8 5.8 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4785711 182414 None 0 Mouse Functional pKd = 5.8 5.8 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 976 12 9 10 -0.9 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
137632948 156582 None 0 Mouse Functional pKd = 5.8 5.8 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4068643 156582 None 0 Mouse Functional pKd = 5.8 5.8 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
155532232 171705 None 0 Mouse Functional pKd = 5.8 5.8 - 2
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 992 12 11 11 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4466724 171705 None 0 Mouse Functional pKd = 5.8 5.8 - 2
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 992 12 11 11 -1.5 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
164608927 184457 None 0 Mouse Functional pKd = 5.8 5.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4846677 184457 None 0 Mouse Functional pKd = 5.8 5.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164622957 186114 None 0 Mouse Functional pKd = 5.8 5.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4871777 186114 None 0 Mouse Functional pKd = 5.8 5.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL501679 214143 None 0 Mouse Functional pKd = 6.8 6.8 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
145949639 162757 None 0 Mouse Functional pKd = 7.7 7.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1049 16 13 11 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4171666 162757 None 0 Mouse Functional pKd = 7.7 7.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1049 16 13 11 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.8b00684
164625246 186033 None 0 Mouse Functional pKd = 7.7 7.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4870667 186033 None 0 Mouse Functional pKd = 7.7 7.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
137654791 158918 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1053 14 10 10 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4095539 158918 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1053 14 10 10 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL264190 210608 None 1 Mouse Functional pKd = 6.7 6.7 -35 8
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=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(N)=O 10.1021/jm800291b
CHEMBL454736 213997 None 0 Mouse Functional pKd = 6.7 6.7 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
145956526 162192 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 929 13 10 10 -0.8 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4162603 162192 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 929 13 10 10 -0.8 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
145960041 162286 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 945 14 11 11 -1.8 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4164111 162286 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 945 14 11 11 -1.8 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
137638391 156858 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4071633 156858 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
164608927 184457 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4846677 184457 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613114 185253 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4858442 185253 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623350 185899 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4868611 185899 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164628715 186497 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4877266 186497 None 0 Mouse Functional pKd = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
137642804 158371 None 0 Mouse Functional pKd = 5.7 5.7 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 832 18 8 6 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4089759 158371 None 0 Mouse Functional pKd = 5.7 5.7 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 832 18 8 6 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
137631920 156436 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 976 12 9 9 0.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4066929 156436 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 976 12 9 9 0.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00856
137632506 156524 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1049 12 10 9 1.6 C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4067947 156524 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1049 12 10 9 1.6 C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
164616496 185392 None 0 Mouse Functional pKd = 5.7 5.7 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860703 185392 None 0 Mouse Functional pKd = 5.7 5.7 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623596 185474 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4862028 185474 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164626062 186600 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4878799 186600 None 0 Mouse Functional pKd = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL2370695 209912 None 0 Mouse Functional pKd = 5.7 5.7 - 2
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
164613361 184777 None 0 Mouse Functional pKd = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4851302 184777 None 0 Mouse Functional pKd = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164610096 184861 None 0 Mouse Functional pKd = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852476 184861 None 0 Mouse Functional pKd = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL2323794 209520 None 0 Mouse Functional pKd = 7.6 7.6 - 3
Antagonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAntagonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
164620572 185771 None 0 Mouse Functional pKd = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866496 185771 None 0 Mouse Functional pKd = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164625782 186481 None 0 Mouse Functional pKd = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4876953 186481 None 0 Mouse Functional pKd = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
145959370 162007 None 0 Mouse Functional pKd = 6.6 6.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 959 14 11 11 -2.3 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4159541 162007 None 0 Mouse Functional pKd = 6.6 6.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 959 14 11 11 -2.3 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
164613712 185349 None 0 Mouse Functional pKd = 6.6 6.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860080 185349 None 0 Mouse Functional pKd = 6.6 6.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623596 185474 None 0 Mouse Functional pKd = 6.6 6.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4862028 185474 None 0 Mouse Functional pKd = 6.6 6.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
10101361 155703 None 0 Mouse Functional pKd = 5.6 5.6 - 4
Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL405174 155703 None 0 Mouse Functional pKd = 5.6 5.6 - 4
Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
162647356 179680 None 0 Mouse Functional pKd = 5.6 5.6 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -1.2 CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4743564 179680 None 0 Mouse Functional pKd = 5.6 5.6 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -1.2 CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O 10.1021/acsmedchemlett.9b00641
137633477 156595 None 0 Mouse Functional pKd = 5.6 5.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4068777 156595 None 0 Mouse Functional pKd = 5.6 5.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
137646614 157538 None 0 Mouse Functional pKd = 5.6 5.6 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4080138 157538 None 0 Mouse Functional pKd = 5.6 5.6 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
137646086 157894 None 0 Mouse Functional pKd = 5.6 5.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4084136 157894 None 0 Mouse Functional pKd = 5.6 5.6 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 908 19 8 6 3.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
164615544 184664 None 0 Mouse Functional pKd = 5.6 5.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4849756 184664 None 0 Mouse Functional pKd = 5.6 5.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL502093 214149 None 0 Mouse Functional pKd = 7.5 7.5 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL103817 208459 None 0 Mouse Functional pKd = 6.5 6.5 -100 4
Agonist activity of compound towards mouse Melanocortin-3 receptor (mMC3R); partial agonistAgonist activity of compound towards mouse Melanocortin-3 receptor (mMC3R); partial agonist
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
122184633 122432 None 0 Human Functional pKd = 8.5 8.5 -1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 122432 None 0 Human Functional pKd = 8.5 8.5 -1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
164610510 184595 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848870 184595 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164612091 184599 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848905 184599 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613261 184603 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848948 184603 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
127035019 136436 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735607 136436 None 0 Mouse Functional pKd = 8.5 8.5 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL413573 213075 None 0 Human Functional pKd = 8.4 8.4 1 4
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
132938008 159513 None 0 Mouse Functional pKd = 6.5 6.5 -1659 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4102048 159513 None 0 Mouse Functional pKd = 6.5 6.5 -1659 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
145952946 162485 None 0 Mouse Functional pKd = 7.5 7.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 999 16 12 10 -0.5 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4167239 162485 None 0 Mouse Functional pKd = 7.5 7.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 999 16 12 10 -0.5 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
145954663 162657 None 0 Mouse Functional pKd = 7.5 7.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 985 15 12 10 -0.9 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4169872 162657 None 0 Mouse Functional pKd = 7.5 7.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 985 15 12 10 -0.9 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
164613261 184603 None 0 Mouse Functional pKd = 7.5 7.5 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848948 184603 None 0 Mouse Functional pKd = 7.5 7.5 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
132938008 159513 None 0 Mouse Functional pKd = 6.5 6.5 -1659 5
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4102048 159513 None 0 Mouse Functional pKd = 6.5 6.5 -1659 5
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
145958585 162339 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 931 13 11 11 -2.2 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4164846 162339 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 931 13 11 11 -2.2 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
145973163 163084 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1007 14 11 11 -1.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4176668 163084 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1007 14 11 11 -1.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
155561116 174973 None 0 Mouse Functional pKd = 6.5 6.5 -208 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 174973 None 0 Mouse Functional pKd = 6.5 6.5 -208 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
137633477 156595 None 0 Mouse Functional pKd = 6.5 6.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4068777 156595 None 0 Mouse Functional pKd = 6.5 6.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
162653604 180495 None 0 Mouse Functional pKd = 5.5 5.5 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4753150 180495 None 0 Mouse Functional pKd = 5.5 5.5 - 0
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O 10.1021/acsmedchemlett.9b00641
164625246 186033 None 0 Mouse Functional pKd = 5.5 5.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4870667 186033 None 0 Mouse Functional pKd = 5.5 5.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
137656661 159725 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1000 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4104582 159725 None 0 Mouse Functional pKd = 6.5 6.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1000 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL501394 214137 None 0 Mouse Functional pKd = 7.4 7.4 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL322610 211234 None 0 Mouse Functional pKd = 7.4 7.4 - 4
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164610510 184595 None 0 Mouse Functional pKd = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848870 184595 None 0 Mouse Functional pKd = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164612217 184845 None 0 Mouse Functional pKd = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852297 184845 None 0 Mouse Functional pKd = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
137639030 156945 None 0 Mouse Functional pKd = 6.4 6.4 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 963 11 10 10 -0.7 C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4072662 156945 None 0 Mouse Functional pKd = 6.4 6.4 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 963 11 10 10 -0.7 C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
137659513 159250 None 0 Mouse Functional pKd = 5.4 5.4 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4099096 159250 None 0 Mouse Functional pKd = 5.4 5.4 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
155546131 173530 None 0 Mouse Functional pKd = 5.4 5.4 -15 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4531291 173530 None 0 Mouse Functional pKd = 5.4 5.4 -15 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
44445085 97074 None 0 Human Functional pKd = 8.3 8.3 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 97074 None 0 Human Functional pKd = 8.3 8.3 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
164617040 185309 None 0 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4859395 185309 None 0 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164613676 185449 None 0 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4861645 185449 None 0 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164624484 185586 None 0 Mouse Functional pKd = 8.3 8.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863587 185586 None 0 Mouse Functional pKd = 8.3 8.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL266417 210683 None 0 Human Functional pKd = 8.3 8.3 -83 6
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL428801 213472 None 0 Human Functional pKd = 8.3 8.3 -26 5
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 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/jm00018a005
CHEMBL3577981 211749 None 1 Mouse Functional pKd = 6.3 6.3 -245 5
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
145952883 162415 None 0 Mouse Functional pKd = 6.3 6.3 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 973 15 11 11 -1.9 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4166050 162415 None 0 Mouse Functional pKd = 6.3 6.3 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 973 15 11 11 -1.9 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL3577981 211749 None 1 Mouse Functional pKd = 6.3 6.3 -245 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
164613712 185349 None 0 Mouse Functional pKd = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860080 185349 None 0 Mouse Functional pKd = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164616496 185392 None 0 Mouse Functional pKd = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860703 185392 None 0 Mouse Functional pKd = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164619441 186146 None 0 Mouse Functional pKd = 6.3 6.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 854 18 6 6 4.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872238 186146 None 0 Mouse Functional pKd = 6.3 6.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 854 18 6 6 4.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
137657385 159766 None 0 Mouse Functional pKd = 5.3 5.3 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4105142 159766 None 0 Mouse Functional pKd = 5.3 5.3 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL 867 21 11 7 0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL322610 211234 None 0 Mouse Functional pKd = 7.3 7.3 - 4
Agonist activity of compound towards mouse Melanocortin-3 receptor (mMC3R)Agonist activity of compound towards mouse Melanocortin-3 receptor (mMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL3600912 211821 None 0 Human Functional pKd = 8.2 8.2 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
164619091 186186 None 0 Mouse Functional pKd = 8.2 8.2 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872732 186186 None 0 Mouse Functional pKd = 8.2 8.2 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
145951686 162956 None 0 Mouse Functional pKd = 7.2 7.2 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 979 13 11 11 -1.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4174761 162956 None 0 Mouse Functional pKd = 7.2 7.2 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 979 13 11 11 -1.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
164610096 184861 None 0 Mouse Functional pKd = 7.2 7.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852476 184861 None 0 Mouse Functional pKd = 7.2 7.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
145951904 162939 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 957 14 10 10 -0.9 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4174361 162939 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 957 14 10 10 -0.9 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
137649684 157138 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 992 13 11 11 -2.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4075125 157138 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 992 13 11 11 -2.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.7b00856
164618743 185590 None 0 Mouse Functional pKd = 6.2 6.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863637 185590 None 0 Mouse Functional pKd = 6.2 6.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164620572 185771 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866496 185771 None 0 Mouse Functional pKd = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
127047624 139896 None 0 Mouse Functional pKd = 6.1 6.1 -123 3
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1054 36 12 13 -0.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799408 139896 None 0 Mouse Functional pKd = 6.1 6.1 -123 3
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1054 36 12 13 -0.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
162650385 180071 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
CHEMBL4747952 180071 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC3R assessed as antagonist potency by alphascreen cAMP assay
ChEMBL 948 11 9 10 -0.8 C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.9b00641
145957356 161988 None 0 Mouse Functional pKd = 7.1 7.1 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1035 15 13 11 -1.9 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4159229 161988 None 0 Mouse Functional pKd = 7.1 7.1 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1035 15 13 11 -1.9 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.8b00684
145953129 162440 None 0 Mouse Functional pKd = 7.1 7.1 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1001 16 13 11 -1.9 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4166449 162440 None 0 Mouse Functional pKd = 7.1 7.1 - 0
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 1001 16 13 11 -1.9 CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
145954673 162671 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 915 12 10 10 -1.2 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4170160 162671 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 915 12 10 10 -1.2 CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.8b00684
145951839 162875 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
CHEMBL4173301 162875 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.8b00684
164613361 184777 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4851302 184777 None 0 Mouse Functional pKd = 7.1 7.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
137632217 156302 None 0 Mouse Functional pKd = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 900 10 10 10 -2.4 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4065443 156302 None 0 Mouse Functional pKd = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 900 10 10 10 -2.4 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00856
137633477 156595 None 0 Mouse Functional pKd = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4068777 156595 None 0 Mouse Functional pKd = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
155544852 174939 None 0 Mouse Functional pKd = 6.1 6.1 -1230 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 174939 None 0 Mouse Functional pKd = 6.1 6.1 -1230 5
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
164613114 185253 None 0 Mouse Functional pKd = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4858442 185253 None 0 Mouse Functional pKd = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164617040 185309 None 0 Mouse Functional pKd = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4859395 185309 None 0 Mouse Functional pKd = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
44310103 166647 None 0 Mouse Functional pKd = 8.1 8.1 - 1
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4237 51 50 66 -10.2 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
77231882 166647 None 0 Mouse Functional pKd = 8.1 8.1 - 1
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4237 51 50 66 -10.2 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL428134 166647 None 0 Mouse Functional pKd = 8.1 8.1 - 1
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL 4237 51 50 66 -10.2 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
127047336 139798 None 0 Mouse Functional pKd = 6.1 6.1 -33 4
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798768 139798 None 0 Mouse Functional pKd = 6.1 6.1 -33 4
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
127046262 139820 None 0 Mouse Functional pKd = 6.1 6.1 -45 3
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1012 35 12 13 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798912 139820 None 0 Mouse Functional pKd = 6.1 6.1 -45 3
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1012 35 12 13 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL103817 208459 None 0 Mouse Functional pKd = 6.0 6.0 -100 4
Antagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC3R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
164619641 185726 None 0 Mouse Functional pKi = 9 9.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4865888 185726 None 0 Mouse Functional pKi = 9 9.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164613340 184720 None 0 Mouse Functional pKi = 8.8 8.8 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4850510 184720 None 0 Mouse Functional pKi = 8.8 8.8 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
127035019 136436 None 0 Mouse Functional pKi = 8.8 8.8 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735607 136436 None 0 Mouse Functional pKi = 8.8 8.8 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
164620129 185747 None 0 Mouse Functional pKi = 8 8.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866219 185747 None 0 Mouse Functional pKi = 8 8.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613340 184720 None 0 Mouse Functional pKi = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4850510 184720 None 0 Mouse Functional pKi = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164626062 186600 None 0 Mouse Functional pKi = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4878799 186600 None 0 Mouse Functional pKi = 7 7.0 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164619091 186186 None 0 Mouse Functional pKi = 6 6.0 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872732 186186 None 0 Mouse Functional pKi = 6 6.0 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164625782 186481 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4876953 186481 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164612091 184599 None 0 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848905 184599 None 0 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613676 185449 None 0 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4861645 185449 None 0 Mouse Functional pKi = 6.9 6.9 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164619641 185726 None 0 Mouse Functional pKi = 7.8 7.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4865888 185726 None 0 Mouse Functional pKi = 7.8 7.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164618743 185590 None 0 Mouse Functional pKi = 7.8 7.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863637 185590 None 0 Mouse Functional pKi = 7.8 7.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164624484 185586 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863587 185586 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164620129 185747 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866219 185747 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164608927 184457 None 0 Mouse Functional pKi = 5.8 5.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4846677 184457 None 0 Mouse Functional pKi = 5.8 5.8 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164622957 186114 None 0 Mouse Functional pKi = 5.8 5.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4871777 186114 None 0 Mouse Functional pKi = 5.8 5.8 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164612217 184845 None 0 Mouse Functional pKi = 8.7 8.7 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852297 184845 None 0 Mouse Functional pKi = 8.7 8.7 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164613361 184777 None 0 Mouse Functional pKi = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4851302 184777 None 0 Mouse Functional pKi = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164610096 184861 None 0 Mouse Functional pKi = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852476 184861 None 0 Mouse Functional pKi = 8.6 8.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164625246 186033 None 0 Mouse Functional pKi = 7.7 7.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4870667 186033 None 0 Mouse Functional pKi = 7.7 7.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164608927 184457 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4846677 184457 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 767 18 7 6 4.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613114 185253 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4858442 185253 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623350 185899 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4868611 185899 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164628715 186497 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4877266 186497 None 0 Mouse Functional pKi = 6.7 6.7 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164616496 185392 None 0 Mouse Functional pKi = 5.7 5.7 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860703 185392 None 0 Mouse Functional pKi = 5.7 5.7 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623596 185474 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4862028 185474 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164626062 186600 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4878799 186600 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 795 18 9 6 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164620572 185771 None 0 Mouse Functional pKi = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866496 185771 None 0 Mouse Functional pKi = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164625782 186481 None 0 Mouse Functional pKi = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4876953 186481 None 0 Mouse Functional pKi = 7.6 7.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164613712 185349 None 0 Mouse Functional pKi = 6.6 6.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860080 185349 None 0 Mouse Functional pKi = 6.6 6.6 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164623596 185474 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4862028 185474 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 843 18 7 6 3.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
10101361 155703 None 0 Mouse Functional pKi = 5.6 5.6 - 4
Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL405174 155703 None 0 Mouse Functional pKi = 5.6 5.6 - 4
Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)Agonist activity of compound in mouse Melanocortin-3 receptor (mMC3R)
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
164615544 184664 None 0 Mouse Functional pKi = 5.6 5.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4849756 184664 None 0 Mouse Functional pKi = 5.6 5.6 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL322610 211234 None 0 Mouse Functional pKi = 6.6 6.6 - 4
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL501394 214137 None 0 Mouse Functional pKi = 6.6 6.6 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164610510 184595 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848870 184595 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164612091 184599 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848905 184599 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613261 184603 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848948 184603 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
127035019 136436 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735607 136436 None 0 Mouse Functional pKi = 8.5 8.5 - 1
Partial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisPartial agonist activity at mouse MC3 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis
ChEMBL 1074 17 14 11 0.1 CCCCC(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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
164613261 184603 None 0 Mouse Functional pKi = 7.5 7.5 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848948 184603 None 0 Mouse Functional pKi = 7.5 7.5 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 889 20 9 7 0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
137633477 156595 None 0 Mouse Functional pKi = 6.5 6.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4068777 156595 None 0 Mouse Functional pKi = 6.5 6.5 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164625246 186033 None 0 Mouse Functional pKi = 5.5 5.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4870667 186033 None 0 Mouse Functional pKi = 5.5 5.5 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 726 20 10 7 0.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL502093 214149 None 0 Mouse Functional pKi = 6.5 6.5 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164610510 184595 None 0 Mouse Functional pKi = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4848870 184595 None 0 Mouse Functional pKi = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164612217 184845 None 0 Mouse Functional pKi = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852297 184845 None 0 Mouse Functional pKi = 7.4 7.4 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 830 20 12 7 -0.5 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164617040 185309 None 0 Mouse Functional pKi = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4859395 185309 None 0 Mouse Functional pKi = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164613676 185449 None 0 Mouse Functional pKi = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4861645 185449 None 0 Mouse Functional pKi = 8.3 8.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164624484 185586 None 0 Mouse Functional pKi = 8.3 8.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863587 185586 None 0 Mouse Functional pKi = 8.3 8.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 754 20 12 7 0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
164613712 185349 None 0 Mouse Functional pKi = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860080 185349 None 0 Mouse Functional pKi = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 958 18 8 6 2.8 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164616496 185392 None 0 Mouse Functional pKi = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4860703 185392 None 0 Mouse Functional pKi = 6.3 6.3 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 806 18 8 6 3.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164619441 186146 None 0 Mouse Functional pKi = 6.3 6.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 854 18 6 6 4.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872238 186146 None 0 Mouse Functional pKi = 6.3 6.3 - 0
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 854 18 6 6 4.2 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL454736 213997 None 0 Mouse Functional pKi = 5.3 5.3 - 2
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164619091 186186 None 0 Mouse Functional pKi = 8.2 8.2 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4872732 186186 None 0 Mouse Functional pKi = 8.2 8.2 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL501679 214143 None 0 Mouse Functional pKi = 5.2 5.2 - 3
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
164610096 184861 None 0 Mouse Functional pKi = 7.2 7.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4852476 184861 None 0 Mouse Functional pKi = 7.2 7.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 813 20 9 7 1.1 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164618743 185590 None 0 Mouse Functional pKi = 6.2 6.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4863637 185590 None 0 Mouse Functional pKi = 6.2 6.2 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 737 20 9 7 1.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164620572 185771 None 0 Mouse Functional pKi = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4866496 185771 None 0 Mouse Functional pKi = 6.2 6.2 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 802 20 10 7 0.4 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.1c01417
164613361 184777 None 0 Mouse Functional pKi = 7.1 7.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4851302 184777 None 0 Mouse Functional pKi = 7.1 7.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
137633477 156595 None 0 Mouse Functional pKi = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4068777 156595 None 0 Mouse Functional pKi = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164613114 185253 None 0 Mouse Functional pKi = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4858442 185253 None 0 Mouse Functional pKi = 6.1 6.1 - 0
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 882 18 8 6 3.3 CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.1c01417
164617040 185309 None 0 Mouse Functional pKi = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
CHEMBL4859395 185309 None 0 Mouse Functional pKi = 6.1 6.1 - 1
Antagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis
ChEMBL 765 20 11 7 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.1c01417
131839615 212636 None 26 Mouse Functional pEC50 = 8.0 8.0 -1 7
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 assayAgonist 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
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
16133835 212636 None 26 Mouse Functional pEC50 = 8.0 8.0 -1 7
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 assayAgonist 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
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
CHEMBL407070 212636 None 26 Mouse Functional pEC50 = 8.0 8.0 -1 7
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 assayAgonist 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
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
10408 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
5329 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379.0 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
CHEMBL2070241 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
DB11653 720 None 28 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
6546 3075 None 0 Human Functional pIC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17482720
1334 1501 None 7 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
16133814 1501 None 7 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
CHEMBL437050 1501 None 7 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
1341 3076 None 0 Human Functional pIC50 = 9.7 9.7 -6 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1329 314 None 0 Mouse Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
1335 315 None 0 Human Functional pIC50 None 7.7 7.7 -39 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9819197




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

1971 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 38 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
216416 111581 None 48 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111581 None 48 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
71496458 115564 None 87 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115564 None 87 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
135409453 3773 None 41 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 41 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 41 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
214 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 58 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2435 3590 None 83 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 83 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 83 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 83 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 83 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
25181577 78219 None 56 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78219 None 56 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
4046 2483 None 33 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 33 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 33 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 33 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
176 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157.0 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 398 None 66 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2351 4300 None 49 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4300 None 49 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4300 None 49 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
1046 202652 None 116 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
CHEMBL614 202652 None 116 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
156419 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
156419.0 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 938 None 74 Human Binding pAC50 = 4.9 4.9 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
4212 198679 None 82 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL1417019 198679 None 82 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL58 198679 None 82 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
41684 31221 None 105 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31221 None 105 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
154257 178619 None 67 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178619 None 67 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
104850 3330 None 96 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 None 96 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 None 96 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 None 96 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 None 96 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
24826799 10798 None 104 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10798 None 104 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2162 41514 None 100 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41514 None 100 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3926 207241 None 40 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 207241 None 40 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
4046 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4046 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 33 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
42890 9425 None 59 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9425 None 59 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
11980903 14492 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14492 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14492 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14492 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5440 28724 None 37 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28724 None 37 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28724 None 37 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28724 None 37 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2194 63083 None 101 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
CHEMBL178862 63083 None 101 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
5328940 100216 None 107 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 100216 None 107 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
1212 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372.0 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1662 None 50 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3380 22790 None 34 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
CHEMBL13280 22790 None 34 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
1427 2013 None 54 Human Binding pAC50 = 4.7 4.7 - 27
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 54 Human Binding pAC50 = 4.7 4.7 - 27
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 54 Human Binding pAC50 = 4.7 4.7 - 27
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 54 Human Binding pAC50 = 4.7 4.7 - 27
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 54 Human Binding pAC50 = 4.7 4.7 - 27
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
4046 2483 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4011 82408 None 49 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82408 None 49 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
2726 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 68 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2519 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
2519.0 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
407 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
463 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL113 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
DB00201 779 None 86 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
11626560 200937 None 94 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 200937 None 94 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
11976 920 None 59 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 920 None 59 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467.0 920 None 59 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 920 None 59 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 920 None 59 Human Binding pAC50 = 4.7 4.7 - 24
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
1056 3371 None 116 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2405 3371 None 116 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
77999 3371 None 116 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
CHEMBL121 3371 None 116 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
DB00412 3371 None 116 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2200 20203 None 61 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2200.0 20203 None 61 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 20203 None 61 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 20203 None 61 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
DB08799 20203 None 61 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
25382 9157 None 37 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9157 None 37 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
51755 57406 None 54 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1651990 57406 None 54 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
4236 28096 None 66 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1373 28096 None 66 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
103 4153 None 61 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 None 61 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 None 61 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 None 61 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 None 61 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
202 1508 None 77 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1508 None 77 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1508 None 77 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1508 None 77 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1508 None 77 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
180 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 56 Human Binding pAC50 = 4.6 4.6 - 40
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
124087 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 114 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
3676 205270 None 101 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 234 5 1 2 2.6 CCN(CC)CC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
CHEMBL79 205270 None 101 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 234 5 1 2 2.6 CCN(CC)CC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
216239 23795 None 118 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1200485 23795 None 118 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1336 23795 None 118 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
2247 505 None 81 Human Binding pAC50 = 4.6 4.6 -147 42
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 81 Human Binding pAC50 = 4.6 4.6 -147 42
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 81 Human Binding pAC50 = 4.6 4.6 -147 42
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 81 Human Binding pAC50 = 4.6 4.6 -147 42
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 81 Human Binding pAC50 = 4.6 4.6 -147 42
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
26987 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
26987.0 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 949 None 33 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL4743867 214033 None 14 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
3149 12614 None 15 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12614 None 15 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
1353 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 93 Human Binding pAC50 = 4.6 4.6 - 83
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
4150 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019.0 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 788 None 39 Human Binding pAC50 = 4.6 4.6 - 11
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5284550 41721 None 15 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5284550.0 41721 None 15 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41721 None 15 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41721 None 15 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41721 None 15 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
10184665 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
10184665.0 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3991 None 51 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
123631 207400 None 129 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 8 1 7 4.3 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL939 207400 None 129 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 8 1 7 4.3 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1 10.1038/s41467-023-40064-9
135398737 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 93 Human Binding pAC50 = 4.6 4.6 - 89
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
5282175 14432 None 36 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1200661 14432 None 36 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
11511120 78394 None 86 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL2110732 78394 None 86 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
3191 102858 None 97 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3191.0 102858 None 97 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102858 None 97 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102858 None 97 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
25077405 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
25077405.0 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3902 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
49800011.0 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1201309 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00666 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
2398 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 62 Human Binding pAC50 = 4.6 4.6 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
10184653 10997 None 107 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
CHEMBL1173655 10997 None 107 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
2585 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2585.0 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 None 103 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
30323 62485 None 57 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62485 None 57 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62485 None 57 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2286 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927.0 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 None 51 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
6436173 55116 None 45 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55116 None 45 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
2713 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 205271 None 82 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
72093 35061 None 9 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35061 None 9 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35061 None 9 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
73348210.0 210949 None 0 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
CHEMBL3039583 210949 None 0 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
2600 3779 None 74 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 74 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 74 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 74 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 74 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1209 1658 None 75 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 75 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 75 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 75 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 75 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
1222 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396.0 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1664 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
2335 11848 None 22 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11848 None 22 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11848 None 22 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11848 None 22 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
5329102 194726 None 86 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194726 None 86 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
68617 205527 None 62 Human Binding pAC50 = 5.1 5.1 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205527 None 62 Human Binding pAC50 = 5.1 5.1 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205527 None 62 Human Binding pAC50 = 5.1 5.1 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
1016 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3747 None 78 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
4746 204891 None 31 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 204891 None 31 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 204891 None 31 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
118422671 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562.0 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301.0 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194.0 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2757 None 65 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
16362 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16362.0 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 None 71 Human Binding pAC50 = 5.0 5.0 - 30
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
100 3805 None 58 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 58 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 58 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 58 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 58 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2274 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917.0 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 None 58 Human Binding pAC50 = 5.0 5.0 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
1155 1629 None 53 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
3343 1629 None 53 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
557 1629 None 53 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL32800 1629 None 53 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
DB01288 1629 None 53 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
1324 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
16154396 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727.0 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
44285019 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
57514683 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
91898441 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL441738 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
DB04931 302 None 25 Mouse Binding pEC50 = 10.1 10.1 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16154396 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727.0 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44285019 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
57514683 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
91898441 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL441738 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
DB04931 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
1324 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
16154396 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727.0 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
44285019 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
57514683 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
91898441 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
CHEMBL441738 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
DB04931 302 None 25 Mouse Binding pEC50 = 10.0 10.0 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None None 10.1021/jm0104872
1323 2688 None 55 Mouse Binding pEC50 = 9.9 9.9 - 3
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
92432 2688 None 55 Mouse Binding pEC50 = 9.9 9.9 - 3
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL430239 2688 None 55 Mouse Binding pEC50 = 9.9 9.9 - 3
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16154396 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16197727 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16197727.0 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
44285019 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
57514683 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
91898441 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL441738 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
DB04931 302 None 25 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
1323 2688 None 55 Mouse Binding pEC50 = 9.8 9.8 - 3
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
92432 2688 None 55 Mouse Binding pEC50 = 9.8 9.8 - 3
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL430239 2688 None 55 Mouse Binding pEC50 = 9.8 9.8 - 3
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44327392 141863 None 0 Mouse Binding pEC50 = 9.8 9.8 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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 141863 None 0 Mouse Binding pEC50 = 9.8 9.8 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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 55 Human Binding pEC50 = 9.6 9.6 -72 3
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
92432 2688 None 55 Human Binding pEC50 = 9.6 9.6 -72 3
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL430239 2688 None 55 Human Binding pEC50 = 9.6 9.6 -72 3
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
1323 2688 None 55 Mouse Binding pEC50 = 9.5 9.5 - 3
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
92432 2688 None 55 Mouse Binding pEC50 = 9.5 9.5 - 3
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL430239 2688 None 55 Mouse Binding pEC50 = 9.5 9.5 - 3
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
16132144 209279 None 36 Mouse Binding pEC50 = 9.2 9.2 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 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/jm049010r
16133793 209279 None 36 Mouse Binding pEC50 = 9.2 9.2 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 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/jm049010r
44273719 209279 None 36 Mouse Binding pEC50 = 9.2 9.2 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 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/jm049010r
CHEMBL214332 209279 None 36 Mouse Binding pEC50 = 9.2 9.2 - 4
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 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/jm049010r
16132144 209279 None 36 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 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 209279 None 36 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 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 209279 None 36 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 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
CHEMBL214332 209279 None 36 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 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
16132144 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
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/jm020296e
16133793 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
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/jm020296e
44273719 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
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/jm020296e
CHEMBL214332 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
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/jm020296e
16132144 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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/jm0104872
16133793 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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/jm0104872
44273719 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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/jm0104872
CHEMBL214332 209279 None 36 Mouse Binding pEC50 = 9.1 9.1 - 4
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 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/jm0104872
CHEMBL2369959 209740 None 0 Mouse Binding pEC50 = 9.0 9.0 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)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](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2370154 209801 None 0 Human Binding pEC50 = 8.7 8.7 -1 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
44323211 107018 None 0 Human Binding pEC50 = 6 6.0 - 1
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL315397 107018 None 0 Human Binding pEC50 = 6 6.0 - 1
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432201 213633 None 0 Mouse Binding pEC50 = 5.0 5.0 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL96871 215921 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL327479 211294 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
44323233 106716 None 0 Human Binding pEC50 = 7.9 7.9 -4 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 106716 None 0 Human Binding pEC50 = 7.9 7.9 -4 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL2369972 209753 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL347364 211713 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
CHEMBL2369970 209751 None 0 Mouse Binding pEC50 = 4.9 4.9 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369983 209764 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)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](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL94369 215908 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL154251 208801 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL320157 211226 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
44369234 45246 None 0 Mouse Binding pEC50 = 6.8 6.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL152612 45246 None 0 Mouse Binding pEC50 = 6.8 6.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL264190 210608 None 1 Mouse Binding pEC50 = 6.8 6.8 -39 2
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=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(N)=O 10.1021/jm0104872
CHEMBL188738 209059 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190551 209066 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL358833 211803 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL347216 211712 None 0 Mouse Binding pEC50 = 5.8 5.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
CHEMBL348901 211716 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/jm020296e
11038873 171880 None 0 Human Binding pEC50 = 5.8 5.8 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL446941 171880 None 0 Human Binding pEC50 = 5.8 5.8 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL2369976 209757 None 0 Mouse Binding pEC50 = 4.8 4.8 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
44323020 168996 None 0 Human Binding pEC50 = 7.8 7.8 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 168996 None 0 Human Binding pEC50 = 7.8 7.8 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL431092 213622 None 0 Mouse Binding pEC50 = 4.7 4.7 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL188459 209057 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL372237 212172 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL346925 211711 None 0 Mouse Binding pEC50 = 4.7 4.7 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
44269189 98338 None 0 Human Binding pEC50 = 5.7 5.7 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL275067 98338 None 0 Human Binding pEC50 = 5.7 5.7 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL317968 211207 None 0 Mouse Binding pEC50 = 5.6 5.6 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2096693 209204 None 0 Mouse Binding pEC50 = 4.6 4.6 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/jm020296e
CHEMBL2369969 209750 None 0 Mouse Binding pEC50 = 4.6 4.6 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL373344 212175 None 0 Human Binding pEC50 = 7.6 7.6 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
44269217 30260 None 0 Human Binding pEC50 = 6.6 6.6 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL13910 30260 None 0 Human Binding pEC50 = 6.6 6.6 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL152986 208797 None 0 Mouse Binding pEC50 = 4.6 4.6 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm020296e
CHEMBL2369967 209748 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL330561 211333 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](Cc1cccs1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
1325 3600 None 14 Mouse Binding pEC50 = 8.5 8.5 -12 7
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
6440621 3600 None 14 Mouse Binding pEC50 = 8.5 8.5 -12 7
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
9898183 3600 None 14 Mouse Binding pEC50 = 8.5 8.5 -12 7
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL3422426 3600 None 14 Mouse Binding pEC50 = 8.5 8.5 -12 7
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL349795 211720 None 0 Mouse Binding pEC50 = 4.5 4.5 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccs1)C(N)=O 10.1021/jm020296e
CHEMBL2369977 209758 None 0 Mouse Binding pEC50 = 4.5 4.5 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL186970 209054 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL191120 209080 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL365262 212037 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL2369982 209763 None 0 Mouse Binding pEC50 = 6.5 6.5 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369975 209756 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2371147 210017 None 0 Mouse Binding pEC50 = 4.5 4.5 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
CHEMBL2369966 209747 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL154153 208800 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm020296e
CHEMBL151906 208794 None 0 Mouse Binding pEC50 = 5.4 5.4 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(N)=O 10.1021/jm020296e
44269214 98494 None 0 Human Binding pEC50 = 5.4 5.4 - 0
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276012 98494 None 0 Human Binding pEC50 = 5.4 5.4 - 0
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL2369962 209743 None 0 Mouse Binding pEC50 = 4.4 4.4 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL365794 212041 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL370321 212167 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44323212 168719 None 0 Human Binding pEC50 = 4.4 4.4 1 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=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](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 168719 None 0 Human Binding pEC50 = 4.4 4.4 1 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=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](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL2369965 209746 None 0 Mouse Binding pEC50 = 6.4 6.4 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
137635396 155850 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
Agonist activity at mouse MC3RAgonist activity at mouse MC3R
ChEMBL 1607 50 22 21 -4.6 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)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)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.7b00301
CHEMBL4060118 155850 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
Agonist activity at mouse MC3RAgonist activity at mouse MC3R
ChEMBL 1607 50 22 21 -4.6 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)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)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.7b00301
CHEMBL2369963 209744 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL190080 209062 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL190953 209077 None 0 Human Binding pEC50 = 5.3 5.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2371829 210134 None 0 Human Binding pEC50 = 5.3 5.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL152555 208795 None 0 Mouse Binding pEC50 = 4.3 4.3 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C(N)=O)C(c1ccccc1)c1ccccc1 10.1021/jm020296e
CHEMBL264190 210608 None 1 Mouse Binding pEC50 = 5.3 5.3 -39 2
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=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(N)=O 10.1021/jm020296e
CHEMBL2304247 209484 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Displacement of MT2 from mouse MC3R expressed in HEK293 cellsDisplacement of MT2 from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL3350327 211470 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Displacement of MT2 from mouse MC3R expressed in HEK293 cellsDisplacement of MT2 from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
CHEMBL2369964 209745 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL94391 215909 None 0 Mouse Binding pEC50 = 5.2 5.2 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL191063 209079 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL189991 209061 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL190732 209067 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL264190 210608 None 1 Mouse Binding pEC50 = 7.2 7.2 -39 2
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None CC(=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(N)=O 10.1021/ml500340z
10260053 168203 None 0 Human Binding pEC50 = 7.2 7.2 4 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 168203 None 0 Human Binding pEC50 = 7.2 7.2 4 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL365913 212043 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44323234 168056 None 0 Human Binding pEC50 = 7.2 7.2 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 168056 None 0 Human Binding pEC50 = 7.2 7.2 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322795 206926 None 0 Human Binding pEC50 = 7.2 7.2 -13 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 206926 None 0 Human Binding pEC50 = 7.2 7.2 -13 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11813437 98529 None 0 Human Binding pEC50 = 5.2 5.2 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276301 98529 None 0 Human Binding pEC50 = 5.2 5.2 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL357558 211743 None 0 Mouse Binding pEC50 = 6.1 6.1 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm020296e
44322869 106160 None 0 Human Binding pEC50 = 7.1 7.1 6 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 106160 None 0 Human Binding pEC50 = 7.1 7.1 6 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
46877881 201818 None 0 Human Binding pEC50 = 6.1 6.1 -2 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 201818 None 0 Human Binding pEC50 = 6.1 6.1 -2 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL190203 209064 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL330233 211331 None 0 Mouse Binding pEC50 = 5.1 5.1 - 0
In vitro activation of mouse recombinant Melanocortin-3 receptor.In vitro activation of mouse recombinant Melanocortin-3 receptor.
ChEMBL None None None CC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0104872
CHEMBL2371147 210017 None 0 Mouse Binding pEC50 = 5 5.0 - 0
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cellsActivity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1 10.1021/jm020296e
CHEMBL1161322 208508 None 0 Human Binding pIC50 = 9.7 9.7 -1 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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]2CCCN2C1=O 10.1021/jm0202526
44366081 10262 None 0 Human Binding pIC50 = 9.7 9.7 -2 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 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]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10262 None 0 Human Binding pIC50 = 9.7 9.7 -2 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 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]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 209206 None 0 Human Binding pIC50 = 9.6 9.6 -5 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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/jm0202526
CHEMBL500743 214124 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
1324 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
1324 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 25 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
1323 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
1323 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
145972289 164520 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 164520 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44418421 168593 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL435923 168593 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL393075 212462 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](N)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](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
1323 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
92432 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
1323 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
92432 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
1323 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.9 8.9 -72 3
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL204310 209164 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0510326
122184576 122428 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 122428 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413573 213075 None 0 Human Binding pIC50 = 8.8 8.8 -1 2
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
CHEMBL428801 213472 None 0 Human Binding pIC50 = 8.7 8.7 -100 3
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 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/jm00018a005
1323 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
133053557 163706 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 163706 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
118735101 118801 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118801 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL410795 212842 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
118735103 118803 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118803 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44315095 103133 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL307857 103133 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
155544852 174939 None 0 Mouse Binding pIC50 = 5 5.0 -31 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4565367 174939 None 0 Mouse Binding pIC50 = 5 5.0 -31 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 977 12 10 10 -0.5 CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL410217 212808 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)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)NC1=O 10.1021/jm960845e
127047853 139993 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1948 72 23 25 -2.1 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799955 139993 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1948 72 23 25 -2.1 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
44448629 167463 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167463 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
122184635 122434 None 0 Human Binding pIC50 = 7.0 7.0 1 4
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122434 None 0 Human Binding pIC50 = 7.0 7.0 1 4
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 163834 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 163834 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44445083 154305 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 154305 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
145948876 167483 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 167483 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 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]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161316 208504 None 0 Human Binding pIC50 = 7.0 7.0 -63 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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)C2(CCCC2)NC1=O 10.1021/jm0202526
6918813 131371 None 3 Human Binding pIC50 = 6.0 6.0 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131371 None 3 Human Binding pIC50 = 6.0 6.0 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
24774602 168931 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 168931 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2096710 209205 None 0 Mouse Binding pIC50 = 4.9 4.9 - 1
Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 3 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 3 Receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049620r
44445085 97074 None 0 Human Binding pIC50 = 7.9 7.9 -2 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 97074 None 0 Human Binding pIC50 = 7.9 7.9 -2 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL425591 213338 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
10304547 168252 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL433764 168252 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL382369 212305 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
44448479 155371 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 155371 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
176 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL373344 212175 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL188459 209057 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190203 209064 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL3578004 211758 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.5b00184
122184909 122554 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122554 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL203760 209161 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0510326
122184638 122437 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 122437 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
71449047 78480 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 78480 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
127047624 139896 None 0 Mouse Binding pIC50 = 5.9 5.9 -177 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1054 36 12 13 -0.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799408 139896 None 0 Mouse Binding pIC50 = 5.9 5.9 -177 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1054 36 12 13 -0.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
127046235 139638 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1004 36 12 13 -1.3 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3797690 139638 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1004 36 12 13 -1.3 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.5b01894
10188529 126781 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL365401 126781 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL3350396 211479 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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)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)NC1=O 10.1021/jm960845e
145964837 164347 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[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/acs.jmedchem.8b00488
CHEMBL4212629 164347 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[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/acs.jmedchem.8b00488
CHEMBL2373991 210381 None 0 Mouse Binding pIC50 = 6.9 6.9 -5 2
Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 3 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 3 Receptor
ChEMBL None None None CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/jm049620r
CHEMBL263822 210590 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL383250 212312 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
CHEMBL2371962 210159 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
CHEMBL103817 208459 None 0 Mouse Binding pIC50 = 5.8 5.8 -52 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
122184634 122433 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 122433 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44448660 94973 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 94973 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44449216 95271 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL256286 95271 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600912 211821 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44366171 121294 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 121294 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
127053936 152240 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3968918 152240 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
155546131 173530 None 0 Mouse Binding pIC50 = 4.8 4.8 -10 3
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4531291 173530 None 0 Mouse Binding pIC50 = 4.8 4.8 -10 3
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 929 9 8 10 -0.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
2247 505 None 81 Human Binding pIC50 = 4.8 4.8 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Human Binding pIC50 = 4.8 4.8 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Human Binding pIC50 = 4.8 4.8 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Human Binding pIC50 = 4.8 4.8 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Human Binding pIC50 = 4.8 4.8 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL186970 209054 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
145973975 164657 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164657 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
6918813 131371 None 3 Human Binding pIC50 = 5.8 5.8 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131371 None 3 Human Binding pIC50 = 5.8 5.8 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
71456245 78976 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 78976 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
122184911 122556 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122556 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184575 122427 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 122427 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
10282847 122965 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360819 122965 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL3577981 211749 None 1 Mouse Binding pIC50 = 4.8 4.8 -31 3
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
5624 32693 None 14 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32693 None 14 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32693 None 14 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
57854192 153049 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 153049 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
127053937 149053 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL3942822 149053 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
4189 206922 None 96 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
1338 3807 None 43 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 43 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 43 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
16132144 209279 None 36 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
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 10.1016/j.bmcl.2005.05.109
16133793 209279 None 36 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
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 10.1016/j.bmcl.2005.05.109
44273719 209279 None 36 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
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 10.1016/j.bmcl.2005.05.109
CHEMBL214332 209279 None 36 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
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 10.1016/j.bmcl.2005.05.109
CHEMBL3600840 211817 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL1161321 208507 None 0 Human Binding pIC50 = 6.7 6.7 -19 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
44577514 172455 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 172455 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL2112008 209226 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2221249 209443 None 0 Human Binding pIC50 = 6.7 6.7 1 3
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O nan
1016 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 None 78 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL365913 212043 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL190427 209065 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL190551 209066 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
1323 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
92432 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
1323 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
1323 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.7 8.7 -72 3
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
CHEMBL503229 214163 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=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)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL443071 213920 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
145967155 164243 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4211275 164243 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL502300 214152 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
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]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2096742 209206 None 0 Human Binding pIC50 = 8.6 8.6 -5 2
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
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/jm801300c
CHEMBL501592 214141 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
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]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL3752534 212216 None 1 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
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]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161320 208506 None 0 Human Binding pIC50 = 8.6 8.6 12 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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)C2(CC2)NC1=O 10.1021/jm0202526
CHEMBL1161323 208509 None 0 Human Binding pIC50 = 8.6 8.6 -5 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
122184637 122436 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 122436 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL204263 209163 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL524861 215623 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
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](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
1324 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
145975465 163949 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 163949 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
122184910 122555 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122555 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24774521 154258 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398635 154258 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600832 211813 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
71456219 78747 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 78747 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44396986 67432 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 67432 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44408287 75386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
15953838 67270 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 67270 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL539306 67270 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
168282779 191171 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5188894 191171 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600920 211823 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145988152 167044 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 167044 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
127053935 144185 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 144185 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL217305 209373 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/s0960-894x(03)00412-8
122184499 122393 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 122393 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
24774438 94855 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253789 94855 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
9808801 60809 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 60809 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
44408286 140668 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 140668 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
6918813 131371 None 3 Human Binding pIC50 = 5.6 5.6 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131371 None 3 Human Binding pIC50 = 5.6 5.6 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
168273822 190570 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 190570 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
122184578 122430 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600839 122430 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL217584 209377 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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)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)NC1=O 10.1021/jm960845e
2726 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
168285801 191481 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 191481 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
44347840 161924 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 161924 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 161924 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL2096759 209208 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2115441 209268 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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)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)NC1=O 10.1021/jm960845e
CHEMBL380638 212271 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
137651071 157467 None 0 Mouse Binding pIC50 = 5.6 5.6 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4079298 157467 None 0 Mouse Binding pIC50 = 5.6 5.6 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 794 15 7 6 1.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
145976444 163963 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[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/acs.jmedchem.8b00488
CHEMBL4207858 163963 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[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/acs.jmedchem.8b00488
CHEMBL3600834 211815 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371966 210163 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL203602 209160 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
CHEMBL381739 212292 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
6918707 104192 None 1 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL309807 104192 None 1 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
155561116 174973 None 0 Mouse Binding pIC50 = 4.6 4.6 -10 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4566163 174973 None 0 Mouse Binding pIC50 = 4.6 4.6 -10 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 964 11 11 11 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
44431512 145924 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)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](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 145924 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)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](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL2372588 210272 None 0 Human Binding pIC50 = 6.5 6.5 -316 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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]2Cc3ccccc3N2C1=O 10.1021/jm0202526
44348144 157822 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 157822 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44349173 116990 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
CHEMBL338768 116990 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
44448631 95070 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95070 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44448590 95599 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95599 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2371712 210109 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44347838 96643 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL263585 96643 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3600835 211816 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2096742 209206 None 0 Human Binding pIC50 = 8.5 8.5 -5 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
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/jm070461w
1324 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727.0 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1324 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 25 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL266417 210683 None 0 Human Binding pIC50 = 8.5 8.5 -8 3
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL3600736 211812 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1324 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727.0 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 302 None 25 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
145964017 164041 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 164041 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
16132144 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
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/jm049579s
16133793 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
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/jm049579s
44273719 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
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/jm049579s
CHEMBL214332 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
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/jm049579s
16132144 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 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/jm030111j
16133793 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 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/jm030111j
44273719 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 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/jm030111j
CHEMBL214332 209279 None 36 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 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/jm030111j
CHEMBL408509 212720 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
168295644 192312 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 192312 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
44348183 97165 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL268094 97165 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44408173 75401 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75401 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL188738 209059 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
6918849 122964 None 1 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360818 122964 None 1 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
163196518 192129 None 2 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 192129 None 2 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
24774519 94854 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253788 94854 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2310901 209498 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
132938008 159513 None 0 Mouse Binding pIC50 = 5.5 5.5 -138 3
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4102048 159513 None 0 Mouse Binding pIC50 = 5.5 5.5 -138 3
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4299619 213595 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None CC(=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)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
54587278 60818 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 60818 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3601426 211826 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
6918276 15611 None 7 Human Binding pIC50 = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 15611 None 7 Human Binding pIC50 = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
137653916 158580 None 0 Mouse Binding pIC50 = 5.5 5.5 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4091894 158580 None 0 Mouse Binding pIC50 = 5.5 5.5 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 828 18 9 8 1.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
127047475 139749 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
132991507 139749 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798421 139749 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1630 54 21 19 -1.2 CC(=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)NCCCOCCOCCOCCCNC(=O)COCC(=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(N)=O 10.1021/acs.jmedchem.5b01894
127047336 139798 None 0 Mouse Binding pIC50 = 6.5 6.5 -52 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798768 139798 None 0 Mouse Binding pIC50 = 6.5 6.5 -52 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1730 54 21 19 1.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
44418430 83255 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218748 83255 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
10077258 15031 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15031 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
3198 205513 None 76 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL3600842 211819 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24857886 155248 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402769 155248 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
24858629 195469 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL552520 195469 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44408155 140553 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140553 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44445082 154302 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 154302 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
54586246 60817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762008 60817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL2371967 210164 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
CHEMBL190732 209067 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL2371835 210137 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL365794 212041 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
1324 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16154396 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727.0 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
44285019 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
57514683 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
91898441 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL441738 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
DB04931 302 None 25 Mouse Binding pIC50 = 8.4 8.4 - 4
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
145973779 164732 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217528 164732 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44577510 188735 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188735 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
1334 1501 None 7 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 7 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 7 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL1775066 208881 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
44408388 140323 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 140323 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44277696 101205 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 101205 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44277696 101205 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 101205 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL1161318 208505 None 0 Human Binding pIC50 = 7.4 7.4 -79 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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)C2(CCCCC2)NC1=O 10.1021/jm0202526
44397220 167304 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 167304 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL3600841 211818 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
137649368 157406 None 0 Mouse Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4078495 157406 None 0 Mouse Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 844 15 7 6 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
15953833 78974 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 78974 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
16725559 94989 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 94989 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
44431513 145809 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)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)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391704 145809 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)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)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
44348200 160196 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 160196 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3348530 211402 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)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)NC1=O 10.1016/j.bmcl.2003.10.056
132180599 156893 None 0 Mouse Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4072129 156893 None 0 Mouse Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 841 20 11 7 0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL2371965 210162 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL439691 213848 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
168296790 192346 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5206941 192346 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
168273291 190532 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179637 190532 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
145987870 167234 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4292317 167234 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44408190 96923 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 96923 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL3600833 211814 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
49862378 15042 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 15042 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
71459938 78981 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 78981 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44397455 123843 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL362523 123843 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL417853 213238 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligandInhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligand
ChEMBL None None None C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(03)00164-1
46919520 15138 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15138 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44408276 75507 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75507 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862425 15060 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 15060 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
155551202 173959 None 0 Mouse Binding pIC50 = 4.3 4.3 - 0
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 895 8 8 10 -0.5 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4541505 173959 None 0 Mouse Binding pIC50 = 4.3 4.3 - 0
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 895 8 8 10 -0.5 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
44418431 136556 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL373821 136556 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL413439 213070 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
145966716 164305 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 164305 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1324 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16154396 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727.0 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
44285019 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
57514683 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
91898441 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL441738 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
DB04931 302 None 25 Mouse Binding pIC50 = 8.3 8.3 - 4
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
44431511 88066 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)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](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL234629 88066 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)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](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL263948 210599 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
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](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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/jm960840h
16132144 209279 None 36 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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/jm960845e
16133793 209279 None 36 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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/jm960845e
44273719 209279 None 36 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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/jm960845e
CHEMBL214332 209279 None 36 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
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/jm960845e
CHEMBL1775062 208880 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
118735100 118800 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 118800 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL191120 209080 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL191063 209079 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL370321 212167 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL264190 210608 None 1 Mouse Binding pIC50 = 4.3 4.3 -39 2
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL None None None CC(=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(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL3600921 211824 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408252 140669 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140669 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
155548853 173809 None 0 Mouse Binding pIC50 = 4.3 4.3 -79 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
CHEMBL4538274 173809 None 0 Mouse Binding pIC50 = 4.3 4.3 -79 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL 1005 13 10 10 -0.6 CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.9b00860
137653704 158633 None 0 Mouse Binding pIC50 = 5.3 5.3 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4092424 158633 None 0 Mouse Binding pIC50 = 5.3 5.3 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 838 18 8 7 2.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL3600913 211822 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145971389 164633 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164633 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
132180598 157849 None 0 Mouse Binding pIC50 = 6.3 6.3 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4083717 157849 None 0 Mouse Binding pIC50 = 6.3 6.3 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL446185 213944 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)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)NC1=O 10.1021/jm0510326
71449048 78481 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 78481 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm030111j
145966490 164362 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 164362 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145948912 167485 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 167485 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
122184914 122559 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122559 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145966364 164120 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 164120 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3754655 212223 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL414778 213156 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438920 213809 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL204864 209166 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
16157270 212553 None 14 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 212553 None 14 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2372589 210273 None 0 Human Binding pIC50 = 8.2 8.2 15 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 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]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
16157270 212553 None 14 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 212553 None 14 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL427205 213352 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
122184912 122558 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122558 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44577520 188824 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 188824 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL411359 212879 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44396987 67193 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL187774 67193 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 78971 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 78971 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71456220 78748 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 78748 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL264190 210608 None 1 Human Binding pIC50 = 7.2 7.2 - 2
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None CC(=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(N)=O 10.1016/j.ejmech.2018.04.021
44408253 140344 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 140344 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL2371963 210160 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL190080 209062 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
168295131 192242 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 192242 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL3600843 211820 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
52918026 60808 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 60808 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
137658359 159571 None 0 Mouse Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4102774 159571 None 0 Mouse Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 791 20 11 7 -1.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.7b00301
10257242 15030 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 15030 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL3601431 211827 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408189 168879 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168879 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
168278924 191066 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 191066 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
1334 1501 None 7 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 7 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 7 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1334 1501 None 7 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 7 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 7 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
145976863 163758 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163758 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
168274393 190105 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5172938 190105 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
54584302 60812 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 60812 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
54584301 60810 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
CHEMBL1761872 60810 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
44408154 141362 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 141362 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
1338 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
9938402 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL339053 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
1338 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 43 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
49862375 15039 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 15039 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL190953 209077 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL275999 210826 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL372237 212172 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
122184577 122429 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 122429 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
122184636 122435 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 122435 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1324 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16154396 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727.0 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
44285019 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
57514683 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
91898441 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
DB04931 302 None 25 Mouse Binding pIC50 = 8.1 8.1 - 4
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
1323 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.1 8.1 -72 3
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL3349030 211405 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL409144 212747 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm0510326
10210964 67243 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL187990 67243 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
44445084 160739 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL411391 160739 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44408275 75419 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75419 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL3799094 212268 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL375947 212232 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
49862377 15041 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 15041 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
11753695 8393 None 7 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8393 None 7 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
122184633 122432 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 122432 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 55 Human Binding pIC50 = 8.0 8.0 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 55 Human Binding pIC50 = 8.0 8.0 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 55 Human Binding pIC50 = 8.0 8.0 -72 3
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
145990599 166855 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 166855 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44397410 124359 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363740 124359 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
1337 3424 None 6 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 6 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 6 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
137639815 156802 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4071063 156802 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 847 20 11 8 0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O 10.1021/acs.jmedchem.7b00301
10304776 78979 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2113041 78979 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
10483153 60811 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 60811 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
132180597 156171 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL4063911 156171 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.7b00301
CHEMBL3600922 211825 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
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)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL389674 212433 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
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](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
127046262 139820 None 0 Mouse Binding pIC50 = 6 6.0 -79 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1012 35 12 13 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798912 139820 None 0 Mouse Binding pIC50 = 6 6.0 -79 3
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
ChEMBL 1012 35 12 13 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
1325 3600 None 14 Mouse Binding pKd = 9.5 9.5 -12 7
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
6440621 3600 None 14 Mouse Binding pKd = 9.5 9.5 -12 7
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
9898183 3600 None 14 Mouse Binding pKd = 9.5 9.5 -12 7
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
CHEMBL3422426 3600 None 14 Mouse Binding pKd = 9.5 9.5 -12 7
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/acs.jmedchem.5b00184
44366081 10262 None 0 Human Binding pKd = 9.4 9.4 -2 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 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]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10262 None 0 Human Binding pKd = 9.4 9.4 -2 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 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]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2372589 210273 None 0 Human Binding pKd = 9.2 9.2 15 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL1161322 208508 None 0 Human Binding pKd = 9 9.0 -1 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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]2CCCN2C1=O 10.1021/jm0202526
1325 3600 None 14 Mouse Binding pKd = 8.7 8.7 -12 7
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL None None None None 10.1021/ml500340z
6440621 3600 None 14 Mouse Binding pKd = 8.7 8.7 -12 7
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL None None None None 10.1021/ml500340z
9898183 3600 None 14 Mouse Binding pKd = 8.7 8.7 -12 7
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL None None None None 10.1021/ml500340z
CHEMBL3422426 3600 None 14 Mouse Binding pKd = 8.7 8.7 -12 7
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL None None None None 10.1021/ml500340z
CHEMBL2096742 209206 None 0 Human Binding pKd = 8.7 8.7 -5 2
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 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/jm0202526
122178168 121261 None 0 Mouse Binding pKd = 7 7.0 -25 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577997 121261 None 0 Mouse Binding pKd = 7 7.0 -25 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577999 211753 None 0 Mouse Binding pKd = 7 7.0 -19 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
122178158 121253 None 0 Mouse Binding pKd = 6 6.0 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577987 121253 None 0 Mouse Binding pKd = 6 6.0 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
122178167 121260 None 0 Mouse Binding pKd = 6.9 6.9 -162 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577996 121260 None 0 Mouse Binding pKd = 6.9 6.9 -162 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
118735609 118880 None 0 Mouse Binding pKd = 5.9 5.9 -251 2
Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422432 118880 None 0 Mouse Binding pKd = 5.9 5.9 -251 2
Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3577980 211748 None 0 Mouse Binding pKd = 5.9 5.9 -7 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
122178169 121262 None 0 Mouse Binding pKd = 6.8 6.8 -31 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 977 13 10 10 -0.4 C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577998 121262 None 0 Mouse Binding pKd = 6.8 6.8 -31 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 977 13 10 10 -0.4 C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3578000 211754 None 0 Mouse Binding pKd = 6.7 6.7 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
118735610 118881 None 0 Mouse Binding pKd = 5.7 5.7 -398 2
Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3422433 118881 None 0 Mouse Binding pKd = 5.7 5.7 -398 2
Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 871 18 9 6 2.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/ml500340z
CHEMBL3577995 211752 None 0 Mouse Binding pKd = 7.6 7.6 -6 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL1161320 208506 None 0 Human Binding pKd = 7.6 7.6 12 2
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 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)C2(CC2)NC1=O 10.1021/jm0202526
122178164 121258 None 0 Mouse Binding pKd = 5.6 5.6 -158 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577993 121258 None 0 Mouse Binding pKd = 5.6 5.6 -158 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL1161318 208505 None 0 Human Binding pKd = 6.5 6.5 -79 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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)C2(CCCCC2)NC1=O 10.1021/jm0202526
CHEMBL3577981 211749 None 1 Mouse Binding pKd = 6.4 6.4 -31 3
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL1161321 208507 None 0 Human Binding pKd = 6.4 6.4 -19 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
118735604 118877 None 0 Mouse Binding pKd = 5.4 5.4 -251 2
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL3422427 118877 None 0 Mouse Binding pKd = 5.4 5.4 -251 2
Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis
ChEMBL 860 18 10 6 2.0 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml500340z
CHEMBL440801 213869 None 0 Human Binding pKd = 8.3 8.3 -25 2
pA2 against human melanocortin receptor, hMC3RpA2 against human melanocortin receptor, hMC3R
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
CHEMBL2096742 209206 None 0 Human Binding pKd = 8.3 8.3 -5 2
pA2 value for the compound against human Melanocortin 3 receptorpA2 value for the compound against human Melanocortin 3 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
CHEMBL1161323 208509 None 0 Human Binding pKd = 8.2 8.2 -5 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL3577977 211745 None 0 Mouse Binding pKd = 6.2 6.2 -3 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
CHEMBL3577978 211746 None 0 Mouse Binding pKd = 6.2 6.2 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
CHEMBL3577982 211750 None 0 Mouse Binding pKd = 6.2 6.2 -3 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3578003 211757 None 0 Mouse Binding pKd = 6.2 6.2 - 1
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL1161316 208504 None 0 Human Binding pKd = 6.2 6.2 -63 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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)C2(CCCC2)NC1=O 10.1021/jm0202526
122178157 121252 None 0 Mouse Binding pKd = 6.1 6.1 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577986 121252 None 0 Mouse Binding pKd = 6.1 6.1 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577976 211744 None 0 Mouse Binding pKd = 6.1 6.1 -2 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
CHEMBL3578002 211756 None 0 Mouse Binding pKd = 6.1 6.1 - 1
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](N)[C@@H](C)O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL2372588 210272 None 0 Human Binding pKd = 6.1 6.1 -316 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 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]2Cc3ccccc3N2C1=O 10.1021/jm0202526
162643092 181724 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181724 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181724 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181724 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183053 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183053 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183053 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183053 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183453 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183453 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183453 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183453 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL414718 213151 None 0 Human Binding pKi = 10.0 10.0 -1 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
1325 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
1325 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 14 Human Binding pKi = 9.9 9.9 -5 7
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
162673931 183058 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183058 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 183058 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183058 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL2370968 209971 None 0 Human Binding pKi = 9.7 9.7 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL442504 213916 None 0 Human Binding pKi = 9.6 9.6 -3 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL415165 213176 None 0 Human Binding pKi = 9.6 9.6 -2 5
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
162668987 182590 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182590 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 182590 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182590 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183124 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183124 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183124 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183124 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 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]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 182871 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182871 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 182871 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182871 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183021 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183021 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183021 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183021 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168277761 190300 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175981 190300 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16154396 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727.0 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
44285019 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
57514683 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
91898441 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL441738 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
DB04931 302 None 25 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
162677133 183557 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183557 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183557 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183557 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 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]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1324 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16154396 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16197727 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16197727.0 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
44285019 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
57514683 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
91898441 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL441738 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
DB04931 302 None 25 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL2370964 209967 None 0 Human Binding pKi = 9.1 9.1 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL385465 212351 None 0 Human Binding pKi = 9.0 9.0 -10 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
44415913 79951 None 0 Human Binding pKi = 9 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 79951 None 0 Human Binding pKi = 9 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415914 139270 None 0 Human Binding pKi = 9 9.0 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 139270 None 0 Human Binding pKi = 9 9.0 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415919 141588 None 0 Human Binding pKi = 9.0 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 141588 None 0 Human Binding pKi = 9.0 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL2370154 209801 None 0 Human Binding pKi = 8.9 8.9 -1 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
CHEMBL266879 210706 None 0 Human Binding pKi = 8.8 8.8 -6 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0501432
162665450 182296 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182296 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162665450 182296 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182296 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168273645 190325 None 0 Human Binding pKi = 8.0 8.0 -24 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5176443 190325 None 0 Human Binding pKi = 8.0 8.0 -24 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16172929 213001 None 15 Human Binding pKi = 8.0 8.0 -12 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
CHEMBL412536 213001 None 15 Human Binding pKi = 8.0 8.0 -12 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
168289404 191312 None 0 Human Binding pKi = 8.0 8.0 -15 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 191312 None 0 Human Binding pKi = 8.0 8.0 -15 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
122178168 121261 None 0 Mouse Binding pKi = 7 7.0 -25 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577997 121261 None 0 Mouse Binding pKi = 7 7.0 -25 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 963 12 10 10 -0.7 C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577999 211753 None 0 Mouse Binding pKi = 7 7.0 -19 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL5087814 215119 None 0 Human Binding pKi = 7 7.0 -26 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44400811 68641 None 0 Human Binding pKi = 6 6.0 -416 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL191857 68641 None 0 Human Binding pKi = 6 6.0 -416 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
9915636 66824 None 0 Human Binding pKi = 6 6.0 -58 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186083 66824 None 0 Human Binding pKi = 6 6.0 -58 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
122178158 121253 None 0 Mouse Binding pKi = 6 6.0 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577987 121253 None 0 Mouse Binding pKi = 6 6.0 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44434860 90042 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238159 90042 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL5094168 215479 None 0 Human Binding pKi = 7.0 7.0 -707 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090946 215285 None 0 Human Binding pKi = 7.0 7.0 -75 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44401341 135673 None 0 Human Binding pKi = 5.0 5.0 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL372965 135673 None 0 Human Binding pKi = 5.0 5.0 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
176 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
59149264 76802 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 76802 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 76802 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 76802 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168277916 190677 None 0 Human Binding pKi = 7.9 7.9 -17 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5181812 190677 None 0 Human Binding pKi = 7.9 7.9 -17 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168272660 190433 None 0 Human Binding pKi = 7.9 7.9 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 190433 None 0 Human Binding pKi = 7.9 7.9 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322869 106160 None 0 Human Binding pKi = 7.0 7.0 6 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 106160 None 0 Human Binding pKi = 7.0 7.0 6 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322895 163370 None 0 Human Binding pKi = 7.0 7.0 -18 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 163370 None 0 Human Binding pKi = 7.0 7.0 -18 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285313 191401 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 191401 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44433294 153043 None 0 Human Binding pKi = 6.0 6.0 -575 3
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL397580 153043 None 0 Human Binding pKi = 6.0 6.0 -575 3
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL2070254 209185 None 0 Human Binding pKi = 6.0 6.0 -31 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44397030 67369 None 0 Human Binding pKi = 6.0 6.0 -131 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL188651 67369 None 0 Human Binding pKi = 6.0 6.0 -131 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
6918850 125422 None 1 Human Binding pKi = 6.0 6.0 -316 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
CHEMBL364560 125422 None 1 Human Binding pKi = 6.0 6.0 -316 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
10270570 89033 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236450 89033 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44401592 125190 None 0 Human Binding pKi = 6.0 6.0 -4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL364519 125190 None 0 Human Binding pKi = 6.0 6.0 -4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
46905545 10300 None 0 Human Binding pKi = 5.0 5.0 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161792 10300 None 0 Human Binding pKi = 5.0 5.0 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44415972 79883 None 0 Human Binding pKi = 5.9 5.9 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 79883 None 0 Human Binding pKi = 5.9 5.9 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL5078687 214580 None 0 Human Binding pKi = 5.9 5.9 -75 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845450 138469 None 0 Human Binding pKi = 6.9 6.9 -91 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 138469 None 0 Human Binding pKi = 6.9 6.9 -91 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
51346770 58227 None 0 Human Binding pKi = 5.9 5.9 -10 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
CHEMBL1682209 58227 None 0 Human Binding pKi = 5.9 5.9 -10 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
44413876 79744 None 0 Human Binding pKi = 5.9 5.9 -93 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 79744 None 0 Human Binding pKi = 5.9 5.9 -93 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 79744 None 0 Human Binding pKi = 5.9 5.9 -93 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 79744 None 0 Human Binding pKi = 5.9 5.9 -93 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL2370967 209970 None 0 Human Binding pKi = 7.9 7.9 -2 2
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44323234 168056 None 0 Human Binding pKi = 7.9 7.9 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 168056 None 0 Human Binding pKi = 7.9 7.9 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347331 16327 None 0 Human Binding pKi = 6.9 6.9 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16327 None 0 Human Binding pKi = 6.9 6.9 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
16007264 79720 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL211564 79720 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
16007264 79720 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
CHEMBL211564 79720 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
71452732 79034 None 0 Human Binding pKi = 5.9 5.9 -1 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113139 79034 None 0 Human Binding pKi = 5.9 5.9 -1 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
71461657 79039 None 0 Human Binding pKi = 5.9 5.9 -4 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113144 79039 None 0 Human Binding pKi = 5.9 5.9 -4 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44435220 89252 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236803 89252 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
10293285 89612 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL237528 89612 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
10137615 89736 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237692 89736 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 90030 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90030 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434766 154714 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154714 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
59149266 76926 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693081 76926 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929807 76926 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070250 76926 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168296647 192475 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 192475 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
11845813 139804 None 0 Human Binding pKi = 5.9 5.9 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 139804 None 0 Human Binding pKi = 5.9 5.9 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
1338 3807 None 43 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 43 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 43 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
44413829 78066 None 0 Human Binding pKi = 5.9 5.9 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 78066 None 0 Human Binding pKi = 5.9 5.9 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
25133556 188849 None 0 Human Binding pKi = 6.9 6.9 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 188849 None 0 Human Binding pKi = 6.9 6.9 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
44569175 188822 None 0 Human Binding pKi = 6.9 6.9 -32 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 188822 None 0 Human Binding pKi = 6.9 6.9 -32 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
168277543 190675 None 0 Human Binding pKi = 4.9 4.9 -128 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 190675 None 0 Human Binding pKi = 4.9 4.9 -128 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
59149255 76928 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 76928 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 76928 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 76928 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11993702 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 18 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
168276507 190265 None 0 Human Binding pKi = 7.9 7.9 -33 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 190265 None 0 Human Binding pKi = 7.9 7.9 -33 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322896 167972 None 0 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 167972 None 0 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168293710 192166 None 0 Human Binding pKi = 7.9 7.9 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 192166 None 0 Human Binding pKi = 7.9 7.9 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322958 107012 None 0 Human Binding pKi = 6.9 6.9 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 107012 None 0 Human Binding pKi = 6.9 6.9 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
122178167 121260 None 0 Mouse Binding pKi = 6.9 6.9 -162 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577996 121260 None 0 Mouse Binding pKi = 6.9 6.9 -162 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 948 11 10 10 -1.1 C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44432932 87754 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233758 87754 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44400863 69164 None 0 Human Binding pKi = 5.9 5.9 -288 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192464 69164 None 0 Human Binding pKi = 5.9 5.9 -288 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44456219 155438 None 0 Human Binding pKi = 5.9 5.9 -275 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL403806 155438 None 0 Human Binding pKi = 5.9 5.9 -275 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL3577979 211747 None 0 Mouse Binding pKi = 5.9 5.9 -8 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.5b00184
16046215 80089 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
CHEMBL213122 80089 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
16046215 80089 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
CHEMBL213122 80089 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
44434843 88700 None 0 Human Binding pKi = 4.9 4.9 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 88700 None 0 Human Binding pKi = 4.9 4.9 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434854 90029 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 90029 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434648 148159 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393558 148159 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168285101 191644 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191644 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5080489 214689 None 0 Human Binding pKi = 6.9 6.9 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
2247 505 None 81 Human Binding pKi = 4.9 4.9 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Human Binding pKi = 4.9 4.9 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Human Binding pKi = 4.9 4.9 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Human Binding pKi = 4.9 4.9 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Human Binding pKi = 4.9 4.9 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44401573 71198 None 0 Human Binding pKi = 5.9 5.9 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL195638 71198 None 0 Human Binding pKi = 5.9 5.9 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL420167 213242 None 0 Human Binding pKi = 7.9 7.9 -8 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL266417 210683 None 0 Human Binding pKi = 6.9 6.9 -8 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
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](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
10260053 168203 None 0 Human Binding pKi = 6.9 6.9 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 168203 None 0 Human Binding pKi = 6.9 6.9 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
44322787 105964 None 0 Human Binding pKi = 6.9 6.9 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 105964 None 0 Human Binding pKi = 6.9 6.9 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370965 209968 None 0 Human Binding pKi = 5.9 5.9 -1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44433439 89924 None 0 Human Binding pKi = 5.9 5.9 -165 3
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL237976 89924 None 0 Human Binding pKi = 5.9 5.9 -165 3
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44323212 168719 None 0 Human Binding pKi = 5.9 5.9 1 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=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](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 168719 None 0 Human Binding pKi = 5.9 5.9 1 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=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](Cc2ccccc2)NC1=O 10.1021/jm020021z
11180881 66821 None 1 Human Binding pKi = 5.9 5.9 -93 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
CHEMBL186074 66821 None 1 Human Binding pKi = 5.9 5.9 -93 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
44395681 66870 None 0 Human Binding pKi = 5.9 5.9 -100 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186289 66870 None 0 Human Binding pKi = 5.9 5.9 -100 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44415417 80146 None 0 Human Binding pKi = 5.9 5.9 -12 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL213380 80146 None 0 Human Binding pKi = 5.9 5.9 -12 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
10304463 76774 None 0 Human Binding pKi = 5.9 5.9 -14 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL206840 76774 None 0 Human Binding pKi = 5.9 5.9 -14 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
9915636 66824 None 0 Human Binding pKi = 5.9 5.9 -58 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL186083 66824 None 0 Human Binding pKi = 5.9 5.9 -58 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44265715 10185 None 0 Human Binding pKi = 4.9 4.9 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159702 10185 None 0 Human Binding pKi = 4.9 4.9 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
10108894 89737 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
CHEMBL237693 89737 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
44434697 148693 None 0 Human Binding pKi = 4.9 4.9 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL393994 148693 None 0 Human Binding pKi = 4.9 4.9 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434757 152741 None 0 Human Binding pKi = 4.9 4.9 -7 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397324 152741 None 0 Human Binding pKi = 4.9 4.9 -7 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
25129105 177019 None 0 Human Binding pKi = 6.8 6.8 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 177019 None 0 Human Binding pKi = 6.8 6.8 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL5081077 214717 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44401418 124016 None 0 Human Binding pKi = 5.8 5.8 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL362964 124016 None 0 Human Binding pKi = 5.8 5.8 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413913 138673 None 0 Human Binding pKi = 5.8 5.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 138673 None 0 Human Binding pKi = 5.8 5.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL2370963 209966 None 0 Human Binding pKi = 7.8 7.8 -10 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
162670951 182838 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182838 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162670951 182838 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182838 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 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](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
42630327 155871 None 0 Human Binding pKi = 7.8 7.8 -5 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)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)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155871 None 0 Human Binding pKi = 7.8 7.8 -5 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)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)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL407809 212685 None 0 Human Binding pKi = 7.8 7.8 -56 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[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(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL409049 212745 None 0 Human Binding pKi = 6.8 6.8 -12 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
CHEMBL438235 213759 None 0 Human Binding pKi = 6.8 6.8 1 2
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44347219 16580 None 0 Human Binding pKi = 6.8 6.8 -301 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 16580 None 0 Human Binding pKi = 6.8 6.8 -301 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
44347105 113346 None 0 Human Binding pKi = 5.8 5.8 -13 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL331728 113346 None 0 Human Binding pKi = 5.8 5.8 -13 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44393441 66429 None 0 Human Binding pKi = 4.8 4.8 -1 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL185195 66429 None 0 Human Binding pKi = 4.8 4.8 -1 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434662 88514 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235137 88514 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434781 89904 None 0 Human Binding pKi = 4.8 4.8 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 89904 None 0 Human Binding pKi = 4.8 4.8 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
5624 32693 None 14 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32693 None 14 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32693 None 14 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
44413970 139015 None 0 Human Binding pKi = 4.8 4.8 -34 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 139015 None 0 Human Binding pKi = 4.8 4.8 -34 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413938 138939 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 138939 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44569176 172545 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 172545 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
11846669 80277 None 0 Human Binding pKi = 6.8 6.8 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 80277 None 0 Human Binding pKi = 6.8 6.8 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
168271934 190085 None 0 Human Binding pKi = 7.8 7.8 -9 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 190085 None 0 Human Binding pKi = 7.8 7.8 -9 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
1323 2688 None 55 Human Binding pKi = 7.8 7.8 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 55 Human Binding pKi = 7.8 7.8 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 55 Human Binding pKi = 7.8 7.8 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
44322977 111569 None 0 Human Binding pKi = 6.8 6.8 -2 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 111569 None 0 Human Binding pKi = 6.8 6.8 -2 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
122178169 121262 None 0 Mouse Binding pKi = 6.8 6.8 -31 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 977 13 10 10 -0.4 C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577998 121262 None 0 Mouse Binding pKi = 6.8 6.8 -31 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 977 13 10 10 -0.4 C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44577092 178645 None 0 Human Binding pKi = 6.8 6.8 -144 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467586 178645 None 0 Human Binding pKi = 6.8 6.8 -144 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL427629 213357 None 0 Human Binding pKi = 5.8 5.8 -7 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
24873537 146061 None 0 Human Binding pKi = 5.8 5.8 -138 4
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 146061 None 0 Human Binding pKi = 5.8 5.8 -138 4
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44400661 124339 None 0 Human Binding pKi = 5.8 5.8 -512 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
CHEMBL363641 124339 None 0 Human Binding pKi = 5.8 5.8 -512 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
70693083 76929 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929813 76929 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070253 76929 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44434636 89300 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236841 89300 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
9946241 89432 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237079 89432 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434782 90027 None 0 Human Binding pKi = 4.8 4.8 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238144 90027 None 0 Human Binding pKi = 4.8 4.8 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434693 167347 None 0 Human Binding pKi = 4.8 4.8 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL429451 167347 None 0 Human Binding pKi = 4.8 4.8 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
10211466 168900 None 0 Human Binding pKi = 4.8 4.8 -213 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL438432 168900 None 0 Human Binding pKi = 4.8 4.8 -213 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
4189 206922 None 96 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44409257 140586 None 0 Human Binding pKi = 5.8 5.8 -67 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL381357 140586 None 0 Human Binding pKi = 5.8 5.8 -67 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
25133210 169457 None 0 Human Binding pKi = 6.8 6.8 -13 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 169457 None 0 Human Binding pKi = 6.8 6.8 -13 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL427666 213364 None 0 Human Binding pKi = 6.8 6.8 -60 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O 10.1021/jm0501432
CHEMBL2221249 209443 None 0 Human Binding pKi = 6.8 6.8 1 3
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O nan
168273045 190254 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5175392 190254 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415920 80371 None 0 Human Binding pKi = 7.8 7.8 -13 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 80371 None 0 Human Binding pKi = 7.8 7.8 -13 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44322959 156075 None 0 Human Binding pKi = 6.8 6.8 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 156075 None 0 Human Binding pKi = 6.8 6.8 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132864 172602 None 0 Human Binding pKi = 6.8 6.8 -12 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 172602 None 0 Human Binding pKi = 6.8 6.8 -12 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
25058412 189440 None 0 Human Binding pKi = 5.8 5.8 -208 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL513404 189440 None 0 Human Binding pKi = 5.8 5.8 -208 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434587 89438 None 0 Human Binding pKi = 5.8 5.8 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237094 89438 None 0 Human Binding pKi = 5.8 5.8 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434848 88968 None 0 Human Binding pKi = 4.8 4.8 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL236443 88968 None 0 Human Binding pKi = 4.8 4.8 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44434690 89306 None 0 Human Binding pKi = 4.8 4.8 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89306 None 0 Human Binding pKi = 4.8 4.8 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434713 89596 None 0 Human Binding pKi = 4.8 4.8 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 89596 None 0 Human Binding pKi = 4.8 4.8 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
10109225 154672 None 0 Human Binding pKi = 4.8 4.8 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL399624 154672 None 0 Human Binding pKi = 4.8 4.8 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44409240 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
CHEMBL202699 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
44409240 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44409240 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 74434 None 0 Human Binding pKi = 5.8 5.8 -16 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
1016 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 None 78 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL5075506 214379 None 0 Human Binding pKi = 5.8 5.8 -1348 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137658158 159717 None 0 Human Binding pKi = 4.8 4.8 -63 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159717 None 0 Human Binding pKi = 4.8 4.8 -63 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
1323 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
1323 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 55 Human Binding pKi = 7.7 7.7 -72 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
24180646 148182 None 0 Mouse Binding pKi = 6.8 6.8 -251 8
Binding affinity at mouse MC3RBinding affinity at mouse MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 148182 None 0 Mouse Binding pKi = 6.8 6.8 -251 8
Binding affinity at mouse MC3RBinding affinity at mouse MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
44396002 124774 None 0 Human Binding pKi = 5.8 5.8 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
CHEMBL364215 124774 None 0 Human Binding pKi = 5.8 5.8 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
11181804 128507 None 0 Human Binding pKi = 5.8 5.8 -158 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 128507 None 0 Human Binding pKi = 5.8 5.8 -158 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
23661656 169044 None 0 Human Binding pKi = 5.8 5.8 -323 5
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 169044 None 0 Human Binding pKi = 5.8 5.8 -323 5
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434661 88513 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL235136 88513 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
44434603 89913 None 0 Human Binding pKi = 4.8 4.8 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237935 89913 None 0 Human Binding pKi = 4.8 4.8 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265496 97049 None 0 Human Binding pKi = 4.8 4.8 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 97049 None 0 Human Binding pKi = 4.8 4.8 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
44409379 76522 None 0 Human Binding pKi = 4.7 4.7 -85 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL206018 76522 None 0 Human Binding pKi = 4.7 4.7 -85 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
25132525 176725 None 0 Human Binding pKi = 5.7 5.7 -2 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 176725 None 0 Human Binding pKi = 5.7 5.7 -2 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
168270124 189955 None 0 Human Binding pKi = 7.7 7.7 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 189955 None 0 Human Binding pKi = 7.7 7.7 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL407213 212648 None 0 Human Binding pKi = 6.7 6.7 -44 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=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](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
44577060 188052 None 0 Mouse Binding pKi = 6.7 6.7 -54 8
Binding affinity at mouse MC3RBinding affinity at mouse MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 188052 None 0 Mouse Binding pKi = 6.7 6.7 -54 8
Binding affinity at mouse MC3RBinding affinity at mouse MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
137637711 155846 None 0 Mouse Binding pKi = 6.7 6.7 -74 3
Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 3 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 3 expressed in HEK293 cells after 2 hrs by scintillation counting method
ChEMBL 871 11 14 12 -3.9 C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O 10.1021/acs.jmedchem.7b00856
CHEMBL4060087 155846 None 0 Mouse Binding pKi = 6.7 6.7 -74 3
Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 3 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 3 expressed in HEK293 cells after 2 hrs by scintillation counting method
ChEMBL 871 11 14 12 -3.9 C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O 10.1021/acs.jmedchem.7b00856
44577091 178667 None 0 Human Binding pKi = 6.7 6.7 -56 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467772 178667 None 0 Human Binding pKi = 6.7 6.7 -56 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
10408 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
11490658 64943 None 0 Human Binding pKi = 5.7 5.7 -301 2
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL182277 64943 None 0 Human Binding pKi = 5.7 5.7 -301 2
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL88185 215896 None 0 Human Binding pKi = 5.7 5.7 -11 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11296732 143813 None 0 Human Binding pKi = 5.7 5.7 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL390130 143813 None 0 Human Binding pKi = 5.7 5.7 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
10283036 140243 None 0 Human Binding pKi = 5.7 5.7 -331 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380540 140243 None 0 Human Binding pKi = 5.7 5.7 -331 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
11296732 143813 None 0 Human Binding pKi = 5.7 5.7 -43 3
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL390130 143813 None 0 Human Binding pKi = 5.7 5.7 -43 3
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44434772 88597 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88597 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434621 146305 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL392094 146305 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
9969456 147617 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393125 147617 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434845 147903 None 0 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393350 147903 None 0 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
71454518 79150 None 0 Human Binding pKi = 4.7 4.7 -12 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL2113315 79150 None 0 Human Binding pKi = 4.7 4.7 -12 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
11845444 80067 None 0 Human Binding pKi = 4.7 4.7 -11 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 80067 None 0 Human Binding pKi = 4.7 4.7 -11 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
137631599 156526 None 0 Human Binding pKi = 5.7 5.7 -288 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156526 None 0 Human Binding pKi = 5.7 5.7 -288 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11847001 80228 None 0 Human Binding pKi = 5.7 5.7 -138 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 80228 None 0 Human Binding pKi = 5.7 5.7 -138 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
156010247 177072 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
CHEMBL4633001 177072 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
10408 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
10408 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 28 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
57646411 76921 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 76921 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57646441 76920 None 0 Human Binding pKi = 8.6 8.6 -20 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 76920 None 0 Human Binding pKi = 8.6 8.6 -20 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL408843 212735 None 0 Human Binding pKi = 8.6 8.6 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL2370533 209868 None 0 Human Binding pKi = 7.7 7.7 -9 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL331259 211361 None 0 Human Binding pKi = 7.7 7.7 -70 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
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](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
44323029 207181 None 0 Human Binding pKi = 7.7 7.7 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 207181 None 0 Human Binding pKi = 7.7 7.7 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168284733 191624 None 0 Human Binding pKi = 7.7 7.7 -6 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 191624 None 0 Human Binding pKi = 7.7 7.7 -6 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL3578000 211754 None 0 Mouse Binding pKi = 6.7 6.7 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44577062 193374 None 0 Human Binding pKi = 6.7 6.7 -48 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL525177 193374 None 0 Human Binding pKi = 6.7 6.7 -48 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11296600 122943 None 0 Human Binding pKi = 5.7 5.7 -309 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 122943 None 0 Human Binding pKi = 5.7 5.7 -309 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
10180932 89407 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237051 89407 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434695 89426 None 0 Human Binding pKi = 4.7 4.7 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237070 89426 None 0 Human Binding pKi = 4.7 4.7 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434766 154714 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154714 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
25128749 178470 None 0 Human Binding pKi = 6.7 6.7 -25 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 178470 None 0 Human Binding pKi = 6.7 6.7 -25 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
44416152 81098 None 0 Human Binding pKi = 6.7 6.7 -38 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 81098 None 0 Human Binding pKi = 6.7 6.7 -38 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
25129109 188702 None 0 Human Binding pKi = 6.7 6.7 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 188702 None 0 Human Binding pKi = 6.7 6.7 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
44322812 112382 None 0 Human Binding pKi = 6.7 6.7 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 112382 None 0 Human Binding pKi = 6.7 6.7 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434584 151942 None 0 Human Binding pKi = 5.7 5.7 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL396638 151942 None 0 Human Binding pKi = 5.7 5.7 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 88597 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88597 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434690 89306 None 0 Human Binding pKi = 4.7 4.7 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89306 None 0 Human Binding pKi = 4.7 4.7 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10291369 168922 None 0 Human Binding pKi = 4.7 4.7 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438672 168922 None 0 Human Binding pKi = 4.7 4.7 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
2726 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
25132867 172498 None 0 Human Binding pKi = 6.7 6.7 -6 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 172498 None 0 Human Binding pKi = 6.7 6.7 -6 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44413932 137546 None 0 Human Binding pKi = 6.7 6.7 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 137546 None 0 Human Binding pKi = 6.7 6.7 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL2070244 209184 None 0 Human Binding pKi = 7.7 7.7 -21 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577093 178646 None 0 Human Binding pKi = 6.7 6.7 -275 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467587 178646 None 0 Human Binding pKi = 6.7 6.7 -275 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
11341045 66166 None 0 Human Binding pKi = 5.7 5.7 -123 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 66166 None 0 Human Binding pKi = 5.7 5.7 -123 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
44434760 88517 None 0 Human Binding pKi = 4.7 4.7 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235140 88517 None 0 Human Binding pKi = 4.7 4.7 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434691 89425 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL237069 89425 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434701 89501 None 0 Human Binding pKi = 4.7 4.7 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL237291 89501 None 0 Human Binding pKi = 4.7 4.7 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
44434778 89743 None 0 Human Binding pKi = 4.7 4.7 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89743 None 0 Human Binding pKi = 4.7 4.7 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434655 90022 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238135 90022 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 90030 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90030 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
168283984 191246 None 0 Human Binding pKi = 6.7 6.7 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190172 191246 None 0 Human Binding pKi = 6.7 6.7 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415956 141956 None 0 Human Binding pKi = 4.7 4.7 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 141956 None 0 Human Binding pKi = 4.7 4.7 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44415956 141956 None 0 Human Binding pKi = 4.7 4.7 -17 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 141956 None 0 Human Binding pKi = 4.7 4.7 -17 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44409103 140123 None 0 Human Binding pKi = 7.6 7.6 -2 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
CHEMBL380120 140123 None 0 Human Binding pKi = 7.6 7.6 -2 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
168283616 191239 None 0 Human Binding pKi = 7.6 7.6 -11 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 191239 None 0 Human Binding pKi = 7.6 7.6 -11 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44323015 111433 None 0 Human Binding pKi = 6.6 6.6 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 111433 None 0 Human Binding pKi = 6.6 6.6 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
23635107 91558 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
CHEMBL240571 91558 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
23635107 91558 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240571 91558 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11477853 66894 None 0 Human Binding pKi = 5.6 5.6 -63 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 66894 None 0 Human Binding pKi = 5.6 5.6 -63 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
44562414 176817 None 0 Human Binding pKi = 5.6 5.6 -95 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL460942 176817 None 0 Human Binding pKi = 5.6 5.6 -95 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
1338 3807 None 43 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
9938402 3807 None 43 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL339053 3807 None 43 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
44394079 126765 None 0 Human Binding pKi = 5.6 5.6 -85 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL365278 126765 None 0 Human Binding pKi = 5.6 5.6 -85 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
9867330 97841 None 0 Human Binding pKi = 5.6 5.6 -100 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 97841 None 0 Human Binding pKi = 5.6 5.6 -100 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44397283 67166 None 0 Human Binding pKi = 5.6 5.6 -181 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL187659 67166 None 0 Human Binding pKi = 5.6 5.6 -181 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434692 88525 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235176 88525 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434847 88957 None 0 Human Binding pKi = 4.6 4.6 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236442 88957 None 0 Human Binding pKi = 4.6 4.6 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434778 89743 None 0 Human Binding pKi = 4.6 4.6 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89743 None 0 Human Binding pKi = 4.6 4.6 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434765 161771 None 0 Human Binding pKi = 4.6 4.6 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL413982 161771 None 0 Human Binding pKi = 4.6 4.6 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
137655905 158828 None 0 Human Binding pKi = 4.6 4.6 -64 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158828 None 0 Human Binding pKi = 4.6 4.6 -64 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
16007263 79796 None 0 Human Binding pKi = 6.6 6.6 -41 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 79796 None 0 Human Binding pKi = 6.6 6.6 -41 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
24848995 117947 None 0 Human Binding pKi = 7.6 7.6 11 3
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 117947 None 0 Human Binding pKi = 7.6 7.6 11 3
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL263878 210598 None 0 Human Binding pKi = 6.6 6.6 -1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
44347331 16327 None 0 Human Binding pKi = 6.6 6.6 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16327 None 0 Human Binding pKi = 6.6 6.6 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
24180646 148182 None 0 Rat Binding pKi = 6.6 6.6 -338 8
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 148182 None 0 Rat Binding pKi = 6.6 6.6 -338 8
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
11237444 127465 None 0 Human Binding pKi = 5.6 5.6 -457 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 127465 None 0 Human Binding pKi = 5.6 5.6 -457 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
44397304 126826 None 0 Human Binding pKi = 5.6 5.6 -199 4
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365465 126826 None 0 Human Binding pKi = 5.6 5.6 -199 4
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434764 88560 None 0 Human Binding pKi = 4.6 4.6 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235358 88560 None 0 Human Binding pKi = 4.6 4.6 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434884 88611 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235617 88611 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434689 89175 None 0 Human Binding pKi = 4.6 4.6 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236649 89175 None 0 Human Binding pKi = 4.6 4.6 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10291370 145966 None 0 Human Binding pKi = 4.6 4.6 -28 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391823 145966 None 0 Human Binding pKi = 4.6 4.6 -28 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434762 153010 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 153010 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44409140 141286 None 0 Human Binding pKi = 5.6 5.6 -10 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL383256 141286 None 0 Human Binding pKi = 5.6 5.6 -10 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
44401386 69524 None 0 Human Binding pKi = 5.6 5.6 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL193409 69524 None 0 Human Binding pKi = 5.6 5.6 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
137636677 156100 None 0 Human Binding pKi = 4.6 4.6 -50 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 156100 None 0 Human Binding pKi = 4.6 4.6 -50 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137636965 156216 None 0 Human Binding pKi = 4.6 4.6 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 156216 None 0 Human Binding pKi = 4.6 4.6 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44409337 170461 None 0 Human Binding pKi = 4.6 4.6 -114 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL444883 170461 None 0 Human Binding pKi = 4.6 4.6 -114 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL2370553 209870 None 0 Human Binding pKi = 7.6 7.6 -16 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL3577995 211752 None 0 Mouse Binding pKi = 7.6 7.6 -6 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44401440 70120 None 0 Human Binding pKi = 6.6 6.6 -1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL194011 70120 None 0 Human Binding pKi = 6.6 6.6 -1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
11341046 66880 None 0 Human Binding pKi = 5.6 5.6 -95 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 66880 None 0 Human Binding pKi = 5.6 5.6 -95 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
44562440 179041 None 0 Human Binding pKi = 5.6 5.6 -38 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL471340 179041 None 0 Human Binding pKi = 5.6 5.6 -38 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
122178164 121258 None 0 Mouse Binding pKi = 5.6 5.6 -158 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577993 121258 None 0 Mouse Binding pKi = 5.6 5.6 -158 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
44434880 88610 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235616 88610 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434647 89590 None 0 Human Binding pKi = 4.6 4.6 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
CHEMBL237483 89590 None 0 Human Binding pKi = 4.6 4.6 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
44434767 89735 None 0 Human Binding pKi = 4.6 4.6 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237689 89735 None 0 Human Binding pKi = 4.6 4.6 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434868 149551 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL394669 149551 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434762 153010 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 153010 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434768 154715 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL399811 154715 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
11308054 133616 None 0 Human Binding pKi = 6.6 6.6 -8 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL371365 133616 None 0 Human Binding pKi = 6.6 6.6 -8 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413914 139518 None 0 Human Binding pKi = 7.6 7.6 -40 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 139518 None 0 Human Binding pKi = 7.6 7.6 -40 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
168289457 191380 None 0 Human Binding pKi = 7.6 7.6 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 191380 None 0 Human Binding pKi = 7.6 7.6 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44456222 97925 None 0 Human Binding pKi = 6.6 6.6 -223 3
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 97925 None 0 Human Binding pKi = 6.6 6.6 -223 3
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44323033 107152 None 0 Human Binding pKi = 6.6 6.6 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 107152 None 0 Human Binding pKi = 6.6 6.6 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434694 88601 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235589 88601 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44434761 89167 None 0 Human Binding pKi = 4.6 4.6 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236626 89167 None 0 Human Binding pKi = 4.6 4.6 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434592 89515 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237315 89515 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434682 148604 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393919 148604 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25131477 178701 None 0 Human Binding pKi = 4.6 4.6 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL468252 178701 None 0 Human Binding pKi = 4.6 4.6 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL5075712 214394 None 0 Human Binding pKi = 6.6 6.6 -181 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
57817763 76927 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 76927 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 76927 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 76927 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
23635237 91453 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
CHEMBL240364 91453 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
23635237 91453 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL240364 91453 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
44401513 69162 None 0 Human Binding pKi = 6.6 6.6 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL192450 69162 None 0 Human Binding pKi = 6.6 6.6 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44434581 167051 None 0 Human Binding pKi = 5.6 5.6 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL428903 167051 None 0 Human Binding pKi = 5.6 5.6 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 88597 None 0 Human Binding pKi = 4.6 4.6 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88597 None 0 Human Binding pKi = 4.6 4.6 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434683 89303 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL236847 89303 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
44434769 89739 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237698 89739 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434650 89899 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237910 89899 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434651 89900 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237911 89900 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434654 90021 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238134 90021 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434863 148144 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393552 148144 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168282596 190906 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL5185132 190906 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
168281389 190922 None 0 Human Binding pKi = 7.6 7.6 -7 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=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]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 190922 None 0 Human Binding pKi = 7.6 7.6 -7 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=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]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
44323233 106716 None 0 Human Binding pKi = 6.6 6.6 -4 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 106716 None 0 Human Binding pKi = 6.6 6.6 -4 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322986 106097 None 0 Human Binding pKi = 6.6 6.6 -7 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 106097 None 0 Human Binding pKi = 6.6 6.6 -7 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11249545 66204 None 0 Human Binding pKi = 5.6 5.6 -478 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 66204 None 0 Human Binding pKi = 5.6 5.6 -478 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11364326 66686 None 0 Human Binding pKi = 5.6 5.6 -134 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 66686 None 0 Human Binding pKi = 5.6 5.6 -134 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
24740653 88592 None 0 Human Binding pKi = 5.6 5.6 -758 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL235556 88592 None 0 Human Binding pKi = 5.6 5.6 -758 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
44265707 10184 None 0 Human Binding pKi = 4.6 4.6 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159701 10184 None 0 Human Binding pKi = 4.6 4.6 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434759 88516 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235139 88516 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434688 89173 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236640 89173 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168286369 191712 None 0 Human Binding pKi = 6.6 6.6 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5197030 191712 None 0 Human Binding pKi = 6.6 6.6 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
137640703 157097 None 0 Human Binding pKi = 4.6 4.6 -218 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 157097 None 0 Human Binding pKi = 4.6 4.6 -218 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25133209 173351 None 0 Human Binding pKi = 6.6 6.6 -56 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 173351 None 0 Human Binding pKi = 6.6 6.6 -56 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
25128748 189991 None 0 Human Binding pKi = 5.6 5.6 -28 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 189991 None 0 Human Binding pKi = 5.6 5.6 -28 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL50056 214119 None 2 Human Binding pKi = 5.5 5.5 -41 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm060384p
11845630 139514 None 0 Human Binding pKi = 5.5 5.5 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 139514 None 0 Human Binding pKi = 5.5 5.5 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
11846673 79994 None 0 Human Binding pKi = 6.5 6.5 -3 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 79994 None 0 Human Binding pKi = 6.5 6.5 -3 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44347220 168440 None 0 Human Binding pKi = 7.5 7.5 -112 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 168440 None 0 Human Binding pKi = 7.5 7.5 -112 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL268851 210769 None 0 Human Binding pKi = 7.5 7.5 -33 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44347378 114435 None 0 Human Binding pKi = 5.5 5.5 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333262 114435 None 0 Human Binding pKi = 5.5 5.5 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434772 88597 None 0 Human Binding pKi = 4.5 4.5 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88597 None 0 Human Binding pKi = 4.5 4.5 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
9968756 89509 None 0 Human Binding pKi = 4.5 4.5 -18 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237299 89509 None 0 Human Binding pKi = 4.5 4.5 -18 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434870 148148 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL393553 148148 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44413842 138377 None 0 Human Binding pKi = 4.5 4.5 -18 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 138377 None 0 Human Binding pKi = 4.5 4.5 -18 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL103817 208459 None 0 Mouse Binding pKi = 6.5 6.5 -52 3
Binding constant (Ki) at mouse Melanocortin-3 receptorBinding constant (Ki) at mouse Melanocortin-3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
168278271 191115 None 0 Human Binding pKi = 6.5 6.5 -30 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 191115 None 0 Human Binding pKi = 6.5 6.5 -30 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
6918276 15611 None 7 Human Binding pKi = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 15611 None 7 Human Binding pKi = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL415661 213198 None 0 Human Binding pKi = 8.5 8.5 -21 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[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(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
162643435 181667 None 0 Human Binding pKi = 8.5 8.5 -4 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181667 None 0 Human Binding pKi = 8.5 8.5 -4 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 181667 None 0 Human Binding pKi = 8.5 8.5 -4 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181667 None 0 Human Binding pKi = 8.5 8.5 -4 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44416057 81191 None 0 Human Binding pKi = 8.5 8.5 -3 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 81191 None 0 Human Binding pKi = 8.5 8.5 -3 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
162643518 181711 None 0 Human Binding pKi = 8.4 8.4 -89 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181711 None 0 Human Binding pKi = 8.4 8.4 -89 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 181711 None 0 Human Binding pKi = 8.4 8.4 -89 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181711 None 0 Human Binding pKi = 8.4 8.4 -89 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)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](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1323 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
1323 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 55 Human Binding pKi = 8.4 8.4 -72 3
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
168271899 190601 None 0 Human Binding pKi = 7.5 7.5 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5180727 190601 None 0 Human Binding pKi = 7.5 7.5 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168271237 190488 None 0 Human Binding pKi = 7.5 7.5 -10 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 190488 None 0 Human Binding pKi = 7.5 7.5 -10 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44347379 114436 None 0 Human Binding pKi = 5.5 5.5 -5 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333263 114436 None 0 Human Binding pKi = 5.5 5.5 -5 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347106 115060 None 0 Human Binding pKi = 5.5 5.5 -52 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL334309 115060 None 0 Human Binding pKi = 5.5 5.5 -52 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434872 88564 None 0 Human Binding pKi = 4.5 4.5 -9 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235382 88564 None 0 Human Binding pKi = 4.5 4.5 -9 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434634 89299 None 0 Human Binding pKi = 4.5 4.5 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236840 89299 None 0 Human Binding pKi = 4.5 4.5 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
44434597 89613 None 0 Human Binding pKi = 4.5 4.5 -1 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237530 89613 None 0 Human Binding pKi = 4.5 4.5 -1 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL5080784 214706 None 0 Human Binding pKi = 6.5 6.5 -75 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
25132866 172611 None 0 Human Binding pKi = 6.5 6.5 -77 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL449131 172611 None 0 Human Binding pKi = 6.5 6.5 -77 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
162672691 183201 None 0 Human Binding pKi = 7.5 7.5 -57 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183201 None 0 Human Binding pKi = 7.5 7.5 -57 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672691 183201 None 0 Human Binding pKi = 7.5 7.5 -57 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183201 None 0 Human Binding pKi = 7.5 7.5 -57 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44562287 174248 None 0 Human Binding pKi = 5.5 5.5 -331 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454900 174248 None 0 Human Binding pKi = 5.5 5.5 -331 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
25211670 174260 None 0 Human Binding pKi = 5.5 5.5 -323 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454916 174260 None 0 Human Binding pKi = 5.5 5.5 -323 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
44562460 189265 None 0 Human Binding pKi = 5.5 5.5 -954 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL511826 189265 None 0 Human Binding pKi = 5.5 5.5 -954 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434690 89306 None 0 Human Binding pKi = 4.5 4.5 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89306 None 0 Human Binding pKi = 4.5 4.5 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434713 89596 None 0 Human Binding pKi = 4.5 4.5 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 89596 None 0 Human Binding pKi = 4.5 4.5 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434855 90030 None 0 Human Binding pKi = 4.5 4.5 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90030 None 0 Human Binding pKi = 4.5 4.5 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434859 90034 None 0 Human Binding pKi = 4.5 4.5 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
CHEMBL238158 90034 None 0 Human Binding pKi = 4.5 4.5 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
44265487 97383 None 0 Human Binding pKi = 4.5 4.5 -1 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269689 97383 None 0 Human Binding pKi = 4.5 4.5 -1 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL412494 212997 None 0 Human Binding pKi = 6.5 6.5 -125 3
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
3198 205513 None 76 Human Binding pKi = 4.5 4.5 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Human Binding pKi = 4.5 4.5 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Human Binding pKi = 4.5 4.5 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL5077811 214516 None 0 Human Binding pKi = 5.5 5.5 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
44320339 206123 None 0 Human Binding pKi = 4.5 4.5 -19 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL85918 206123 None 0 Human Binding pKi = 4.5 4.5 -19 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
11845440 138672 None 0 Human Binding pKi = 5.5 5.5 -26 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL377778 138672 None 0 Human Binding pKi = 5.5 5.5 -26 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
24741624 138380 None 0 Human Binding pKi = 6.5 6.5 -22 3
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL377231 138380 None 0 Human Binding pKi = 6.5 6.5 -22 3
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
24741624 138380 None 0 Human Binding pKi = 6.5 6.5 -22 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL377231 138380 None 0 Human Binding pKi = 6.5 6.5 -22 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44397281 126544 None 0 Human Binding pKi = 5.5 5.5 -288 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365237 126544 None 0 Human Binding pKi = 5.5 5.5 -288 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434633 89170 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236630 89170 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25129107 173777 None 0 Human Binding pKi = 6.5 6.5 -36 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 173777 None 0 Human Binding pKi = 6.5 6.5 -36 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
137660993 159447 None 0 Human Binding pKi = 6.5 6.5 -83 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 159447 None 0 Human Binding pKi = 6.5 6.5 -83 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=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)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11156852 65685 None 0 Human Binding pKi = 7.5 7.5 -1 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL183434 65685 None 0 Human Binding pKi = 7.5 7.5 -1 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL408257 212704 None 0 Human Binding pKi = 7.5 7.5 -77 3
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
24740419 148194 None 0 Human Binding pKi = 5.5 5.5 -1318 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
CHEMBL393584 148194 None 0 Human Binding pKi = 5.5 5.5 -1318 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
44434690 89306 None 0 Human Binding pKi = 4.5 4.5 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89306 None 0 Human Binding pKi = 4.5 4.5 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434862 90248 None 0 Human Binding pKi = 4.5 4.5 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238368 90248 None 0 Human Binding pKi = 4.5 4.5 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
10225762 145817 None 0 Human Binding pKi = 4.5 4.5 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL391707 145817 None 0 Human Binding pKi = 4.5 4.5 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434601 146468 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL392223 146468 None 0 Human Binding pKi = 4.5 4.5 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44265374 206488 None 0 Human Binding pKi = 4.5 4.5 -21 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8825 206488 None 0 Human Binding pKi = 4.5 4.5 -21 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
44577060 188052 None 0 Rat Binding pKi = 6.5 6.5 -97 8
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 188052 None 0 Rat Binding pKi = 6.5 6.5 -97 8
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
24180592 97013 None 0 Mouse Binding pKi = 6.5 6.5 -100 6
Binding affinity to mouse MC3RBinding affinity to mouse MC3R
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 97013 None 0 Mouse Binding pKi = 6.5 6.5 -100 6
Binding affinity to mouse MC3RBinding affinity to mouse MC3R
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL2370966 209969 None 0 Human Binding pKi = 5.5 5.5 -28 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
10232787 140381 None 0 Human Binding pKi = 5.5 5.5 -467 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380855 140381 None 0 Human Binding pKi = 5.5 5.5 -467 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44415918 141549 None 0 Human Binding pKi = 7.5 7.5 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 141549 None 0 Human Binding pKi = 7.5 7.5 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
168295726 192405 None 0 Human Binding pKi = 7.5 7.5 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 192405 None 0 Human Binding pKi = 7.5 7.5 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322923 206546 None 0 Human Binding pKi = 6.5 6.5 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 206546 None 0 Human Binding pKi = 6.5 6.5 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11375764 66689 None 0 Human Binding pKi = 5.5 5.5 -1659 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 66689 None 0 Human Binding pKi = 5.5 5.5 -1659 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
24882666 95718 None 0 Human Binding pKi = 5.5 5.5 1 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 385 10 5 3 1.7 N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
CHEMBL258295 95718 None 0 Human Binding pKi = 5.5 5.5 1 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 385 10 5 3 1.7 N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
44393450 123654 None 0 Human Binding pKi = 4.5 4.5 1 3
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362010 123654 None 0 Human Binding pKi = 4.5 4.5 1 3
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44416060 81318 None 0 Human Binding pKi = 6.5 6.5 -58 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 81318 None 0 Human Binding pKi = 6.5 6.5 -58 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
10325955 165271 None 0 Human Binding pKi = 5.4 5.4 -33 4
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 165271 None 0 Human Binding pKi = 5.4 5.4 -33 4
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
11786860 66334 None 1 Human Binding pKi = 5.4 5.4 -281 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185035 66334 None 1 Human Binding pKi = 5.4 5.4 -281 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44434685 89171 None 0 Human Binding pKi = 4.4 4.4 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236638 89171 None 0 Human Binding pKi = 4.4 4.4 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434652 89901 None 0 Human Binding pKi = 4.4 4.4 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237912 89901 None 0 Human Binding pKi = 4.4 4.4 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168289584 191786 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5198158 191786 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168294114 192190 None 0 Human Binding pKi = 7.4 7.4 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5204285 192190 None 0 Human Binding pKi = 7.4 7.4 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44323211 107018 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL315397 107018 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44434666 88559 None 0 Human Binding pKi = 5.4 5.4 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235356 88559 None 0 Human Binding pKi = 5.4 5.4 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
44265672 10181 None 0 Human Binding pKi = 4.4 4.4 -16 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159699 10181 None 0 Human Binding pKi = 4.4 4.4 -16 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44434754 90236 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 90236 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
10292084 148395 None 0 Human Binding pKi = 4.4 4.4 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL393755 148395 None 0 Human Binding pKi = 4.4 4.4 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
25133208 171994 None 0 Human Binding pKi = 6.4 6.4 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 171994 None 0 Human Binding pKi = 6.4 6.4 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
168281969 191278 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 191278 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44322994 106997 None 0 Human Binding pKi = 6.4 6.4 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315258 106997 None 0 Human Binding pKi = 6.4 6.4 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44577063 188100 None 0 Human Binding pKi = 6.4 6.4 -70 4
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL498150 188100 None 0 Human Binding pKi = 6.4 6.4 -70 4
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL5090670 215277 None 0 Human Binding pKi = 6.4 6.4 -37 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44434616 88695 None 0 Human Binding pKi = 4.4 4.4 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236003 88695 None 0 Human Binding pKi = 4.4 4.4 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10159196 89738 None 0 Human Binding pKi = 4.4 4.4 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237694 89738 None 0 Human Binding pKi = 4.4 4.4 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434635 168887 None 0 Human Binding pKi = 4.4 4.4 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438334 168887 None 0 Human Binding pKi = 4.4 4.4 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44409206 140184 None 0 Human Binding pKi = 6.4 6.4 -5 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL380437 140184 None 0 Human Binding pKi = 6.4 6.4 -5 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
11847312 79762 None 0 Human Binding pKi = 5.4 5.4 -6 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 79762 None 0 Human Binding pKi = 5.4 5.4 -6 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL5077095 214479 None 0 Human Binding pKi = 6.4 6.4 -346 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090285 215253 None 0 Human Binding pKi = 6.4 6.4 -138 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137646617 157544 None 0 Human Binding pKi = 4.4 4.4 -8 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 157544 None 0 Human Binding pKi = 4.4 4.4 -8 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46877881 201818 None 0 Human Binding pKi = 6.4 6.4 -2 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 201818 None 0 Human Binding pKi = 6.4 6.4 -2 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44400813 71086 None 0 Human Binding pKi = 6.4 6.4 -134 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195308 71086 None 0 Human Binding pKi = 6.4 6.4 -134 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
9958649 124357 None 0 Human Binding pKi = 5.4 5.4 -354 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 124357 None 0 Human Binding pKi = 5.4 5.4 -354 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
156015336 177519 None 0 Human Binding pKi = 5.4 5.4 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
CHEMBL4639782 177519 None 0 Human Binding pKi = 5.4 5.4 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
44434658 90235 None 0 Human Binding pKi = 4.4 4.4 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 90235 None 0 Human Binding pKi = 4.4 4.4 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434714 148392 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393753 148392 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
137660671 159218 None 0 Human Binding pKi = 5.4 5.4 -416 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 159218 None 0 Human Binding pKi = 5.4 5.4 -416 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
168290510 191897 None 0 Human Binding pKi = 5.4 5.4 -20 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 191897 None 0 Human Binding pKi = 5.4 5.4 -20 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5085972 215003 None 0 Human Binding pKi = 5.4 5.4 -20 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL385556 212354 None 0 Human Binding pKi = 6.4 6.4 -173 3
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL3577981 211749 None 1 Mouse Binding pKi = 6.4 6.4 -31 3
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
10077773 87267 None 4 Human Binding pKi = 6.4 6.4 -204 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233135 87267 None 4 Human Binding pKi = 6.4 6.4 -204 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434850 89174 None 0 Human Binding pKi = 4.4 4.4 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236645 89174 None 0 Human Binding pKi = 4.4 4.4 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
11845276 80053 None 0 Human Binding pKi = 6.4 6.4 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 80053 None 0 Human Binding pKi = 6.4 6.4 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL5076315 214428 None 0 Human Binding pKi = 6.4 6.4 -51 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
168281969 191278 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 191278 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44434657 90234 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 90234 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44415991 80510 None 0 Human Binding pKi = 5.4 5.4 -21 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214770 80510 None 0 Human Binding pKi = 5.4 5.4 -21 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1016/j.bmcl.2006.05.087
44415991 80510 None 0 Human Binding pKi = 5.4 5.4 -21 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1021/jm800525p
CHEMBL214770 80510 None 0 Human Binding pKi = 5.4 5.4 -21 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1021/jm800525p
44413831 78064 None 0 Human Binding pKi = 5.4 5.4 -6 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL210008 78064 None 0 Human Binding pKi = 5.4 5.4 -6 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
57817773 76925 None 0 Human Binding pKi = 7.4 7.4 -245 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684623 76925 None 0 Human Binding pKi = 7.4 7.4 -245 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929806 76925 None 0 Human Binding pKi = 7.4 7.4 -245 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070249 76925 None 0 Human Binding pKi = 7.4 7.4 -245 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44413930 138648 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 138648 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL433645 213643 None 0 Human Binding pKi = 6.4 6.4 -104 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
23635235 166501 None 0 Human Binding pKi = 6.4 6.4 -177 5
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
CHEMBL427860 166501 None 0 Human Binding pKi = 6.4 6.4 -177 5
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
44410803 140172 None 0 Human Binding pKi = 5.4 5.4 -398 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380365 140172 None 0 Human Binding pKi = 5.4 5.4 -398 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44434687 159492 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410179 159492 None 0 Human Binding pKi = 4.4 4.4 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11846844 140079 None 0 Human Binding pKi = 6.4 6.4 -3 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 140079 None 0 Human Binding pKi = 6.4 6.4 -3 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
137653925 158607 None 0 Human Binding pKi = 4.4 4.4 -18 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 158607 None 0 Human Binding pKi = 4.4 4.4 -18 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25128751 173584 None 0 Human Binding pKi = 6.4 6.4 -11 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 173584 None 0 Human Binding pKi = 6.4 6.4 -11 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL438030 213744 None 0 Human Binding pKi = 7.4 7.4 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44434855 90030 None 0 Human Binding pKi = 5.4 5.4 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90030 None 0 Human Binding pKi = 5.4 5.4 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434684 146599 None 0 Human Binding pKi = 4.4 4.4 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392315 146599 None 0 Human Binding pKi = 4.4 4.4 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434665 147949 None 0 Human Binding pKi = 4.4 4.4 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393383 147949 None 0 Human Binding pKi = 4.4 4.4 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25133207 172943 None 0 Human Binding pKi = 6.4 6.4 -16 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
CHEMBL451694 172943 None 0 Human Binding pKi = 6.4 6.4 -16 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
11845438 137623 None 0 Human Binding pKi = 5.4 5.4 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL375775 137623 None 0 Human Binding pKi = 5.4 5.4 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44323034 206530 None 0 Human Binding pKi = 6.4 6.4 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 206530 None 0 Human Binding pKi = 6.4 6.4 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL91957 215905 None 0 Human Binding pKi = 6.4 6.4 -6 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10257541 126342 None 0 Human Binding pKi = 5.4 5.4 -269 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL365039 126342 None 0 Human Binding pKi = 5.4 5.4 -269 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434851 89909 None 0 Human Binding pKi = 4.4 4.4 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237930 89909 None 0 Human Binding pKi = 4.4 4.4 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
10155513 151541 None 0 Human Binding pKi = 4.4 4.4 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396303 151541 None 0 Human Binding pKi = 4.4 4.4 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL2070242 209183 None 0 Human Binding pKi = 7.4 7.4 -9 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44400810 124060 None 0 Human Binding pKi = 6.4 6.4 -316 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 11 3 5 5.4 CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363190 124060 None 0 Human Binding pKi = 6.4 6.4 -316 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 11 3 5 5.4 CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL2070373 209186 None 0 Human Binding pKi = 6.4 6.4 -57 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44434562 88698 None 0 Human Binding pKi = 6.4 6.4 -562 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236014 88698 None 0 Human Binding pKi = 6.4 6.4 -562 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
44577094 178647 None 0 Human Binding pKi = 6.4 6.4 -134 4
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467588 178647 None 0 Human Binding pKi = 6.4 6.4 -134 4
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
1338 3807 None 43 Human Binding pKi = 5.4 5.4 -75 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
9938402 3807 None 43 Human Binding pKi = 5.4 5.4 -75 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL339053 3807 None 43 Human Binding pKi = 5.4 5.4 -75 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
44432964 87453 None 0 Human Binding pKi = 5.4 5.4 -1148 3
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233372 87453 None 0 Human Binding pKi = 5.4 5.4 -1148 3
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44453903 155424 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 387 9 2 5 2.7 N[C@H](Cc1ccc(F)cc1)C(=O)NCCC(Cn1cncn1)C1CCCCC1 10.1016/j.bmcl.2007.11.109
CHEMBL403722 155424 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 387 9 2 5 2.7 N[C@H](Cc1ccc(F)cc1)C(=O)NCCC(Cn1cncn1)C1CCCCC1 10.1016/j.bmcl.2007.11.109
44434865 88750 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL236226 88750 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434690 89905 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237920 89905 None 0 Human Binding pKi = 4.4 4.4 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434849 146856 None 0 Human Binding pKi = 4.4 4.4 -23 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL392521 146856 None 0 Human Binding pKi = 4.4 4.4 -23 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44434614 151584 None 1 Human Binding pKi = 4.4 4.4 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396341 151584 None 1 Human Binding pKi = 4.4 4.4 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265472 206355 None 0 Human Binding pKi = 4.4 4.4 -3 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8742 206355 None 0 Human Binding pKi = 4.4 4.4 -3 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
51346771 58226 None 0 Human Binding pKi = 5.3 5.3 -13 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL1682208 58226 None 0 Human Binding pKi = 5.3 5.3 -13 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
16132144 209279 None 36 Human Binding pKi = 7.3 7.3 -30 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
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/jm201489a
16133793 209279 None 36 Human Binding pKi = 7.3 7.3 -30 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
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/jm201489a
44273719 209279 None 36 Human Binding pKi = 7.3 7.3 -30 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
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/jm201489a
CHEMBL214332 209279 None 36 Human Binding pKi = 7.3 7.3 -30 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
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/jm201489a
44410802 140385 None 0 Human Binding pKi = 5.3 5.3 -263 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380858 140385 None 0 Human Binding pKi = 5.3 5.3 -263 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
44434686 146600 None 0 Human Binding pKi = 4.3 4.3 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL392316 146600 None 0 Human Binding pKi = 4.3 4.3 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
44434698 171025 None 0 Human Binding pKi = 4.3 4.3 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL445669 171025 None 0 Human Binding pKi = 4.3 4.3 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44416122 80128 None 0 Human Binding pKi = 6.3 6.3 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213284 80128 None 0 Human Binding pKi = 6.3 6.3 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
44409104 76525 None 0 Human Binding pKi = 6.3 6.3 -36 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL206033 76525 None 0 Human Binding pKi = 6.3 6.3 -36 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
44347221 16635 None 0 Human Binding pKi = 7.3 7.3 -53 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 16635 None 0 Human Binding pKi = 7.3 7.3 -53 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44416135 80184 None 0 Human Binding pKi = 6.3 6.3 -42 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 80184 None 0 Human Binding pKi = 6.3 6.3 -42 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416135 80184 None 0 Human Binding pKi = 6.3 6.3 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
CHEMBL213566 80184 None 0 Human Binding pKi = 6.3 6.3 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
44434663 88515 None 0 Human Binding pKi = 4.3 4.3 -23 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235138 88515 None 0 Human Binding pKi = 4.3 4.3 -23 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434637 89412 None 0 Human Binding pKi = 4.3 4.3 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237052 89412 None 0 Human Binding pKi = 4.3 4.3 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25129108 172696 None 0 Human Binding pKi = 6.3 6.3 -33 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL450236 172696 None 0 Human Binding pKi = 6.3 6.3 -33 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL5091236 215299 None 0 Human Binding pKi = 6.3 6.3 -602 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL441760 213896 None 0 Human Binding pKi = 6.3 6.3 1 2
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC(C)(C)[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
44265751 106098 None 0 Human Binding pKi = 5.3 5.3 -1 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL313379 106098 None 0 Human Binding pKi = 5.3 5.3 -1 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434611 88614 None 0 Human Binding pKi = 4.3 4.3 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL235627 88614 None 0 Human Binding pKi = 4.3 4.3 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44401392 68657 None 0 Human Binding pKi = 5.3 5.3 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 582 14 5 4 3.1 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL191975 68657 None 0 Human Binding pKi = 5.3 5.3 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 582 14 5 4 3.1 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44577060 188052 None 0 Human Binding pKi = 6.3 6.3 -141 8
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 188052 None 0 Human Binding pKi = 6.3 6.3 -141 8
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434580 151903 None 0 Human Binding pKi = 4.3 4.3 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 335 8 2 2 3.5 NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396598 151903 None 0 Human Binding pKi = 4.3 4.3 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 335 8 2 2 3.5 NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168281421 190957 None 0 Human Binding pKi = 8.3 8.3 -89 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 190957 None 0 Human Binding pKi = 8.3 8.3 -89 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168284256 190946 None 0 Human Binding pKi = 8.3 8.3 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 190946 None 0 Human Binding pKi = 8.3 8.3 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL409636 212773 None 0 Human Binding pKi = 8.3 8.3 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)NC1=O 10.1021/jm030119t
44322868 106008 None 0 Human Binding pKi = 8.2 8.2 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 106008 None 0 Human Binding pKi = 8.2 8.2 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL253364 210509 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](N)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44413931 78015 None 0 Human Binding pKi = 7.3 7.3 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 78015 None 0 Human Binding pKi = 7.3 7.3 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5087839 215120 None 0 Human Binding pKi = 7.3 7.3 -69 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
71458055 79028 None 0 Human Binding pKi = 6.3 6.3 7 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
CHEMBL2113133 79028 None 0 Human Binding pKi = 6.3 6.3 7 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
16038315 138758 None 0 Human Binding pKi = 5.3 5.3 -741 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
CHEMBL378046 138758 None 0 Human Binding pKi = 5.3 5.3 -741 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
44434839 88653 None 0 Human Binding pKi = 4.3 4.3 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235802 88653 None 0 Human Binding pKi = 4.3 4.3 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10157774 89301 None 0 Human Binding pKi = 4.3 4.3 -33 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236842 89301 None 0 Human Binding pKi = 4.3 4.3 -33 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434861 90247 None 0 Human Binding pKi = 4.3 4.3 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238367 90247 None 0 Human Binding pKi = 4.3 4.3 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44413881 137593 None 0 Human Binding pKi = 6.3 6.3 1 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 137593 None 0 Human Binding pKi = 6.3 6.3 1 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
44265751 106098 None 0 Human Binding pKi = 5.3 5.3 -1 3
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL313379 106098 None 0 Human Binding pKi = 5.3 5.3 -1 3
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL5091245 215300 None 0 Human Binding pKi = 5.3 5.3 -120 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
10025669 97392 None 0 Human Binding pKi = 4.3 4.3 -79 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL269776 97392 None 0 Human Binding pKi = 4.3 4.3 -79 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
168276294 190508 None 0 Human Binding pKi = 7.3 7.3 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179373 190508 None 0 Human Binding pKi = 7.3 7.3 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=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]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5087859 215123 None 0 Human Binding pKi = 7.3 7.3 -741 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44434570 89779 None 0 Human Binding pKi = 4.3 4.3 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237719 89779 None 0 Human Binding pKi = 4.3 4.3 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434754 90236 None 0 Human Binding pKi = 4.3 4.3 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 90236 None 0 Human Binding pKi = 4.3 4.3 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44393417 96591 None 0 Human Binding pKi = 5.3 5.3 -13 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL263182 96591 None 0 Human Binding pKi = 5.3 5.3 -13 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434770 88561 None 0 Human Binding pKi = 4.3 4.3 -29 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235359 88561 None 0 Human Binding pKi = 4.3 4.3 -29 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434857 154427 None 0 Human Binding pKi = 4.3 4.3 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398980 154427 None 0 Human Binding pKi = 4.3 4.3 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
71461662 79116 None 0 Human Binding pKi = 4.3 4.3 -4 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2113280 79116 None 0 Human Binding pKi = 4.3 4.3 -4 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
44401607 133617 None 0 Human Binding pKi = 6.3 6.3 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 635 15 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL371366 133617 None 0 Human Binding pKi = 6.3 6.3 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 635 15 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413828 139293 None 0 Human Binding pKi = 6.3 6.3 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 139293 None 0 Human Binding pKi = 6.3 6.3 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
10408 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
5329 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379.0 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
CHEMBL2070241 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
DB11653 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
44265711 206989 None 0 Human Binding pKi = 4.3 4.3 -3 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 206989 None 0 Human Binding pKi = 4.3 4.3 -3 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
23653113 88652 None 0 Human Binding pKi = 4.3 4.3 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235798 88652 None 0 Human Binding pKi = 4.3 4.3 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
137659790 159322 None 0 Human Binding pKi = 4.3 4.3 -102 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 159322 None 0 Human Binding pKi = 4.3 4.3 -102 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44347840 161924 None 0 Human Binding pKi = 7.3 7.3 -17 3
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
91932630 161924 None 0 Human Binding pKi = 7.3 7.3 -17 3
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL415333 161924 None 0 Human Binding pKi = 7.3 7.3 -17 3
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44322788 157383 None 0 Human Binding pKi = 6.3 6.3 -11 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 157383 None 0 Human Binding pKi = 6.3 6.3 -11 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44322957 206211 None 0 Human Binding pKi = 6.3 6.3 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 206211 None 0 Human Binding pKi = 6.3 6.3 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44432966 146301 None 0 Human Binding pKi = 6.3 6.3 -562 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL392092 146301 None 0 Human Binding pKi = 6.3 6.3 -562 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434649 145812 None 0 Human Binding pKi = 5.3 5.3 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 453 12 2 2 6.4 NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391705 145812 None 0 Human Binding pKi = 5.3 5.3 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 453 12 2 2 6.4 NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434653 145815 None 0 Human Binding pKi = 5.3 5.3 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391706 145815 None 0 Human Binding pKi = 5.3 5.3 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434787 148792 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394075 148792 None 0 Human Binding pKi = 5.3 5.3 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL264352 210617 None 0 Human Binding pKi = 7.3 7.3 -104 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
44434696 149198 None 0 Human Binding pKi = 4.3 4.3 -54 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394394 149198 None 0 Human Binding pKi = 4.3 4.3 -54 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44409339 74996 None 0 Human Binding pKi = 4.3 4.3 -1479 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL203252 74996 None 0 Human Binding pKi = 4.3 4.3 -1479 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
44347119 114423 None 0 Human Binding pKi = 7.3 7.3 -151 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 114423 None 0 Human Binding pKi = 7.3 7.3 -151 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL322610 211234 None 0 Mouse Binding pKi = 7.3 7.3 - 1
Binding constant (Ki) at mouse Melanocortin-3 receptorBinding constant (Ki) at mouse Melanocortin-3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
CHEMBL267900 210737 None 0 Human Binding pKi = 7.3 7.3 -144 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
44400934 70613 None 0 Human Binding pKi = 6.3 6.3 -281 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194987 70613 None 0 Human Binding pKi = 6.3 6.3 -281 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44393418 155700 None 0 Human Binding pKi = 5.3 5.3 -5 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL405150 155700 None 0 Human Binding pKi = 5.3 5.3 -5 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44265749 207222 None 0 Human Binding pKi = 4.3 4.3 -6 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 207222 None 0 Human Binding pKi = 4.3 4.3 -6 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
10025669 97392 None 0 Human Binding pKi = 4.3 4.3 -79 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269776 97392 None 0 Human Binding pKi = 4.3 4.3 -79 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
44400660 70730 None 0 Human Binding pKi = 6.2 6.2 -239 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195071 70730 None 0 Human Binding pKi = 6.2 6.2 -239 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44577090 178666 None 0 Human Binding pKi = 6.2 6.2 -57 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467771 178666 None 0 Human Binding pKi = 6.2 6.2 -57 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434598 89816 None 0 Human Binding pKi = 5.2 5.2 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237743 89816 None 0 Human Binding pKi = 5.2 5.2 -1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434867 88523 None 0 Human Binding pKi = 4.2 4.2 -26 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL235162 88523 None 0 Human Binding pKi = 4.2 4.2 -26 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434790 90239 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238353 90239 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265309 205662 None 1 Human Binding pKi = 4.2 4.2 -1 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8201 205662 None 1 Human Binding pKi = 4.2 4.2 -1 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
44400814 70621 None 0 Human Binding pKi = 6.2 6.2 -446 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 627 11 3 5 5.9 O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194990 70621 None 0 Human Binding pKi = 6.2 6.2 -446 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 627 11 3 5 5.9 O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44322987 96732 None 0 Human Binding pKi = 6.2 6.2 -15 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 96732 None 0 Human Binding pKi = 6.2 6.2 -15 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10158674 147915 None 0 Human Binding pKi = 4.2 4.2 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393359 147915 None 0 Human Binding pKi = 4.2 4.2 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265347 96967 None 0 Human Binding pKi = 4.2 4.2 -2 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL266305 96967 None 0 Human Binding pKi = 4.2 4.2 -2 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
23635235 166501 None 0 Human Binding pKi = 6.2 6.2 -177 5
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 166501 None 0 Human Binding pKi = 6.2 6.2 -177 5
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
44347110 114109 None 0 Human Binding pKi = 5.2 5.2 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL332762 114109 None 0 Human Binding pKi = 5.2 5.2 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347082 163908 None 0 Human Binding pKi = 5.2 5.2 -1 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL420727 163908 None 0 Human Binding pKi = 5.2 5.2 -1 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347330 168063 None 0 Human Binding pKi = 5.2 5.2 -1 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432407 168063 None 0 Human Binding pKi = 5.2 5.2 -1 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347081 168627 None 0 Human Binding pKi = 5.2 5.2 -4 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL436169 168627 None 0 Human Binding pKi = 5.2 5.2 -4 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434864 90249 None 0 Human Binding pKi = 4.2 4.2 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238369 90249 None 0 Human Binding pKi = 4.2 4.2 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
2852098 205464 None 13 Human Binding pKi = 4.2 4.2 -4 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8045 205464 None 13 Human Binding pKi = 4.2 4.2 -4 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL439128 213825 None 0 Human Binding pKi = 8.2 8.2 -2 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
CHEMBL412523 213000 None 0 Human Binding pKi = 8.2 8.2 -22 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
44434639 148157 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393557 148157 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44416014 80015 None 0 Human Binding pKi = 5.2 5.2 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212855 80015 None 0 Human Binding pKi = 5.2 5.2 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
44409338 168744 None 0 Human Binding pKi = 5.2 5.2 -1230 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL437132 168744 None 0 Human Binding pKi = 5.2 5.2 -1230 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
44434778 89743 None 0 Human Binding pKi = 4.2 4.2 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89743 None 0 Human Binding pKi = 4.2 4.2 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434853 97204 None 0 Human Binding pKi = 4.2 4.2 -5 2
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 8 2 2 5.3 N[C@@H]1CCCC[C@H]1N(C/C=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL268395 97204 None 0 Human Binding pKi = 4.2 4.2 -5 2
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 8 2 2 5.3 N[C@@H]1CCCC[C@H]1N(C/C=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11215758 66079 None 0 Human Binding pKi = 6.2 6.2 -131 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL183799 66079 None 0 Human Binding pKi = 6.2 6.2 -131 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
44322924 107112 None 0 Human Binding pKi = 6.2 6.2 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316038 107112 None 0 Human Binding pKi = 6.2 6.2 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL3577977 211745 None 0 Mouse Binding pKi = 6.2 6.2 -3 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
CHEMBL3577978 211746 None 0 Mouse Binding pKi = 6.2 6.2 -10 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
CHEMBL3577982 211750 None 0 Mouse Binding pKi = 6.2 6.2 -3 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
10177247 89514 None 0 Human Binding pKi = 4.2 4.2 -5 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237314 89514 None 0 Human Binding pKi = 4.2 4.2 -5 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10200110 89733 None 0 Human Binding pKi = 4.2 4.2 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237687 89733 None 0 Human Binding pKi = 4.2 4.2 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434605 149514 None 0 Human Binding pKi = 4.2 4.2 -9 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
CHEMBL394647 149514 None 0 Human Binding pKi = 4.2 4.2 -9 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
168277258 190710 None 0 Human Binding pKi = 5.2 5.2 -109 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 190710 None 0 Human Binding pKi = 5.2 5.2 -109 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
6918814 127057 None 1 Human Binding pKi = 6.2 6.2 -134 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL365597 127057 None 1 Human Binding pKi = 6.2 6.2 -134 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44433264 89351 None 0 Human Binding pKi = 6.2 6.2 -144 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236940 89351 None 0 Human Binding pKi = 6.2 6.2 -144 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
6918814 127057 None 1 Human Binding pKi = 6.2 6.2 -134 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL365597 127057 None 1 Human Binding pKi = 6.2 6.2 -134 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44265639 10179 None 0 Human Binding pKi = 5.2 5.2 -5 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159697 10179 None 0 Human Binding pKi = 5.2 5.2 -5 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
44434854 90029 None 0 Human Binding pKi = 4.2 4.2 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 90029 None 0 Human Binding pKi = 4.2 4.2 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44323031 168078 None 0 Human Binding pKi = 7.2 7.2 -10 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 168078 None 0 Human Binding pKi = 7.2 7.2 -10 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44397028 124031 None 0 Human Binding pKi = 6.2 6.2 -85 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
CHEMBL363019 124031 None 0 Human Binding pKi = 6.2 6.2 -85 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
44392514 123867 None 0 Human Binding pKi = 5.2 5.2 -7 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362670 123867 None 0 Human Binding pKi = 5.2 5.2 -7 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434794 88520 None 0 Human Binding pKi = 4.2 4.2 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235147 88520 None 0 Human Binding pKi = 4.2 4.2 -4 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434600 148602 None 0 Human Binding pKi = 4.2 4.2 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393918 148602 None 0 Human Binding pKi = 4.2 4.2 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434771 148790 None 0 Human Binding pKi = 4.2 4.2 -30 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394073 148790 None 0 Human Binding pKi = 4.2 4.2 -30 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434572 166592 None 0 Human Binding pKi = 4.2 4.2 -11 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 9 2 2 4.6 NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL428022 166592 None 0 Human Binding pKi = 4.2 4.2 -11 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 9 2 2 4.6 NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44401367 161719 None 0 Human Binding pKi = 7.2 7.2 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL413565 161719 None 0 Human Binding pKi = 7.2 7.2 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44323032 206604 None 0 Human Binding pKi = 7.2 7.2 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 206604 None 0 Human Binding pKi = 7.2 7.2 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434855 90030 None 0 Human Binding pKi = 5.2 5.2 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90030 None 0 Human Binding pKi = 5.2 5.2 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
57817730 76923 None 0 Human Binding pKi = 7.2 7.2 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684622 76923 None 0 Human Binding pKi = 7.2 7.2 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929805 76923 None 0 Human Binding pKi = 7.2 7.2 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070247 76923 None 0 Human Binding pKi = 7.2 7.2 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44400935 70862 None 0 Human Binding pKi = 6.2 6.2 -446 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
CHEMBL195110 70862 None 0 Human Binding pKi = 6.2 6.2 -446 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
44434632 146309 None 0 Human Binding pKi = 4.2 4.2 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392096 146309 None 0 Human Binding pKi = 4.2 4.2 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410168 212804 None 0 Human Binding pKi = 7.2 7.2 -3 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)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)CNC1=O 10.1021/jm030119t
44393421 123103 None 0 Human Binding pKi = 5.2 5.2 -4 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL361052 123103 None 0 Human Binding pKi = 5.2 5.2 -4 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
70684954 77819 None 0 Human Binding pKi = 4.2 4.2 -7 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL2092821 77819 None 0 Human Binding pKi = 4.2 4.2 -7 3
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
9924916 89009 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236447 89009 None 0 Human Binding pKi = 4.2 4.2 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168279695 191135 None 0 Human Binding pKi = 7.2 7.2 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 191135 None 0 Human Binding pKi = 7.2 7.2 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
1334 1501 None 7 Human Binding pKi = 6.2 6.2 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
16133814 1501 None 7 Human Binding pKi = 6.2 6.2 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1501 None 7 Human Binding pKi = 6.2 6.2 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None None 10.1021/jm030119t
44401581 68630 None 0 Human Binding pKi = 6.2 6.2 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL191794 68630 None 0 Human Binding pKi = 6.2 6.2 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44416106 141446 None 0 Human Binding pKi = 8.2 8.2 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 141446 None 0 Human Binding pKi = 8.2 8.2 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44323020 168996 None 0 Human Binding pKi = 8.1 8.1 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 168996 None 0 Human Binding pKi = 8.1 8.1 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL2373515 210379 None 0 Human Binding pKi = 8.1 8.1 -15 3
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
11226756 119974 None 0 Human Binding pKi = 5.2 5.2 -114 3
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 119974 None 0 Human Binding pKi = 5.2 5.2 -114 3
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
6918857 138709 None 1 Human Binding pKi = 5.2 5.2 -239 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL377961 138709 None 1 Human Binding pKi = 5.2 5.2 -239 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
44413880 77946 None 0 Human Binding pKi = 6.2 6.2 -46 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 77946 None 0 Human Binding pKi = 6.2 6.2 -46 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
44401587 10301 None 0 Human Binding pKi = 5.2 5.2 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 611 15 6 5 2.6 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161794 10301 None 0 Human Binding pKi = 5.2 5.2 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 611 15 6 5 2.6 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL5094215 215481 None 0 Human Binding pKi = 6.2 6.2 -60 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2070374 209187 None 0 Human Binding pKi = 7.2 7.2 -123 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
23635236 91601 None 0 Human Binding pKi = 6.2 6.2 -123 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
CHEMBL240780 91601 None 0 Human Binding pKi = 6.2 6.2 -123 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
23635236 91601 None 0 Human Binding pKi = 6.2 6.2 -123 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240780 91601 None 0 Human Binding pKi = 6.2 6.2 -123 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
24180592 97013 None 0 Human Binding pKi = 6.2 6.2 -208 6
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 97013 None 0 Human Binding pKi = 6.2 6.2 -208 6
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44397198 66765 None 0 Human Binding pKi = 6.2 6.2 -93 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL185862 66765 None 0 Human Binding pKi = 6.2 6.2 -93 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434690 89306 None 0 Human Binding pKi = 5.2 5.2 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89306 None 0 Human Binding pKi = 5.2 5.2 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44413832 78065 None 0 Human Binding pKi = 5.1 5.1 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210009 78065 None 0 Human Binding pKi = 5.1 5.1 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
11845804 79558 None 0 Human Binding pKi = 5.1 5.1 -1548 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL211419 79558 None 0 Human Binding pKi = 5.1 5.1 -1548 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
25133907 176724 None 0 Human Binding pKi = 6.1 6.1 -9 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 176724 None 0 Human Binding pKi = 6.1 6.1 -9 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
1338 3807 None 43 Human Binding pKi = 6.1 6.1 -75 4
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
9938402 3807 None 43 Human Binding pKi = 6.1 6.1 -75 4
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
CHEMBL339053 3807 None 43 Human Binding pKi = 6.1 6.1 -75 4
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
10178845 89914 None 0 Human Binding pKi = 5.1 5.1 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237937 89914 None 0 Human Binding pKi = 5.1 5.1 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44413969 80230 None 0 Human Binding pKi = 5.1 5.1 -21 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 80230 None 0 Human Binding pKi = 5.1 5.1 -21 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44415912 139226 None 0 Human Binding pKi = 7.1 7.1 -10 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 139226 None 0 Human Binding pKi = 7.1 7.1 -10 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
24180646 148182 None 0 Human Binding pKi = 6.1 6.1 -1071 8
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 148182 None 0 Human Binding pKi = 6.1 6.1 -1071 8
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
24180646 148182 None 0 Human Binding pKi = 6.1 6.1 -1071 8
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 148182 None 0 Human Binding pKi = 6.1 6.1 -1071 8
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
44434821 90028 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238149 90028 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
137647538 157962 None 0 Human Binding pKi = 5.1 5.1 -1318 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 157962 None 0 Human Binding pKi = 5.1 5.1 -1318 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25131478 169508 None 0 Human Binding pKi = 7.1 7.1 -53 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
CHEMBL443396 169508 None 0 Human Binding pKi = 7.1 7.1 -53 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
44443035 154417 None 0 Human Binding pKi = 6.1 6.1 -1258 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
CHEMBL398929 154417 None 0 Human Binding pKi = 6.1 6.1 -1258 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
44322795 206926 None 0 Human Binding pKi = 7.1 7.1 -13 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 206926 None 0 Human Binding pKi = 7.1 7.1 -13 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL50056 214119 None 2 Human Binding pKi = 6.1 6.1 -41 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
46905544 10299 None 0 Human Binding pKi = 5.1 5.1 4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161791 10299 None 0 Human Binding pKi = 5.1 5.1 4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44434702 149513 None 0 Human Binding pKi = 4.1 4.1 -26 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL394646 149513 None 0 Human Binding pKi = 4.1 4.1 -26 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
44434856 154392 None 0 Human Binding pKi = 4.1 4.1 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398777 154392 None 0 Human Binding pKi = 4.1 4.1 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44400864 124325 None 0 Human Binding pKi = 6.1 6.1 -467 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363576 124325 None 0 Human Binding pKi = 6.1 6.1 -467 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
6918844 168622 None 1 Human Binding pKi = 6.1 6.1 -245 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
CHEMBL436122 168622 None 1 Human Binding pKi = 6.1 6.1 -245 4
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
122178157 121252 None 0 Mouse Binding pKi = 6.1 6.1 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577986 121252 None 0 Mouse Binding pKi = 6.1 6.1 -50 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL 1027 12 10 10 -0.1 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.5b00184
CHEMBL3577976 211744 None 0 Mouse Binding pKi = 6.1 6.1 -2 2
Displacement of MTII from mouse MC3R expressed in HEK293 cellsDisplacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O 10.1021/acs.jmedchem.5b00184
44265496 97049 None 0 Human Binding pKi = 5.1 5.1 -13 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL267020 97049 None 0 Human Binding pKi = 5.1 5.1 -13 4
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
70688853 76924 None 0 Human Binding pKi = 8.1 8.1 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070248 76924 None 0 Human Binding pKi = 8.1 8.1 -23 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57646437 76922 None 0 Human Binding pKi = 8.1 8.1 -74 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684621 76922 None 0 Human Binding pKi = 8.1 8.1 -74 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929804 76922 None 0 Human Binding pKi = 8.1 8.1 -74 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070246 76922 None 0 Human Binding pKi = 8.1 8.1 -74 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
162669632 182565 None 0 Human Binding pKi = 8.1 8.1 -6 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182565 None 0 Human Binding pKi = 8.1 8.1 -6 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162669632 182565 None 0 Human Binding pKi = 8.1 8.1 -6 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182565 None 0 Human Binding pKi = 8.1 8.1 -6 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 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](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
25129453 171766 None 0 Human Binding pKi = 7.1 7.1 -14 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 171766 None 0 Human Binding pKi = 7.1 7.1 -14 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
44400932 70303 None 0 Human Binding pKi = 6.1 6.1 -173 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 588 11 2 6 5.4 CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194393 70303 None 0 Human Binding pKi = 6.1 6.1 -173 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 588 11 2 6 5.4 CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
16007285 81122 None 0 Human Binding pKi = 6.1 6.1 -61 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL215659 81122 None 0 Human Binding pKi = 6.1 6.1 -61 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
44434709 89775 None 0 Human Binding pKi = 4.1 4.1 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237714 89775 None 0 Human Binding pKi = 4.1 4.1 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44400778 135888 None 0 Human Binding pKi = 6.1 6.1 -162 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 574 10 2 6 5.0 COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL373099 135888 None 0 Human Binding pKi = 6.1 6.1 -162 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 574 10 2 6 5.0 COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434785 148791 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394074 148791 None 0 Human Binding pKi = 5.1 5.1 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44413968 80229 None 0 Human Binding pKi = 5.1 5.1 -426 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 80229 None 0 Human Binding pKi = 5.1 5.1 -426 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
24740655 89086 None 0 Human Binding pKi = 6.1 6.1 -1380 4
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
CHEMBL236521 89086 None 0 Human Binding pKi = 6.1 6.1 -1380 4
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
24740655 89086 None 0 Human Binding pKi = 6.1 6.1 -1380 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL236521 89086 None 0 Human Binding pKi = 6.1 6.1 -1380 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
58777892 79044 None 0 Human Binding pKi = 5.1 5.1 -117 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
CHEMBL2113149 79044 None 0 Human Binding pKi = 5.1 5.1 -117 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
44265681 10183 None 0 Human Binding pKi = 4.1 4.1 -28 2
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 369 7 4 4 0.6 NC(N)=NCCCNC(=O)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159700 10183 None 0 Human Binding pKi = 4.1 4.1 -28 2
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 369 7 4 4 0.6 NC(N)=NCCCNC(=O)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44413879 138902 None 0 Human Binding pKi = 6.1 6.1 -64 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 138902 None 0 Human Binding pKi = 6.1 6.1 -64 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
25132526 188923 None 0 Human Binding pKi = 6.1 6.1 -43 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
CHEMBL507876 188923 None 0 Human Binding pKi = 6.1 6.1 -43 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
168279695 191135 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 191135 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44400777 68672 None 0 Human Binding pKi = 6.1 6.1 -295 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 630 13 2 7 4.7 COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192090 68672 None 0 Human Binding pKi = 6.1 6.1 -295 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 630 13 2 7 4.7 COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434763 151343 None 0 Human Binding pKi = 5.1 5.1 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL396111 151343 None 0 Human Binding pKi = 5.1 5.1 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
168285904 191670 None 0 Human Binding pKi = 5.1 5.1 -169 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 191670 None 0 Human Binding pKi = 5.1 5.1 -169 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44413830 77950 None 0 Human Binding pKi = 6.1 6.1 -8 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209622 77950 None 0 Human Binding pKi = 6.1 6.1 -8 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5083551 214869 None 0 Human Binding pKi = 7.1 7.1 -93 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845272 80358 None 0 Human Binding pKi = 7.1 7.1 -8 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 80358 None 0 Human Binding pKi = 7.1 7.1 -8 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44400809 68402 None 0 Human Binding pKi = 6.1 6.1 -407 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 599 11 3 5 5.1 O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL191701 68402 None 0 Human Binding pKi = 6.1 6.1 -407 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 599 11 3 5 5.1 O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
2163781 97377 None 9 Human Binding pKi = 4.1 4.1 -4 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269653 97377 None 9 Human Binding pKi = 4.1 4.1 -4 3
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
44401553 69825 None 0 Human Binding pKi = 6.1 6.1 -18 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 648 14 4 5 3.7 COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.03.120
CHEMBL193715 69825 None 0 Human Binding pKi = 6.1 6.1 -18 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 648 14 4 5 3.7 COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.03.120
25133903 170558 None 0 Human Binding pKi = 5.1 5.1 -15 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
CHEMBL445009 170558 None 0 Human Binding pKi = 5.1 5.1 -15 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
44392535 64272 None 0 Human Binding pKi = 5.1 5.1 -16 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL180937 64272 None 0 Human Binding pKi = 5.1 5.1 -16 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
9960253 116949 None 0 Human Binding pKi = 5.1 5.1 -39 4
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 116949 None 0 Human Binding pKi = 5.1 5.1 -39 4
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
168295173 192311 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 192311 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL89270 215899 None 0 Human Binding pKi = 6.1 6.1 -17 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1016/s0960-894x(03)00552-3
CHEMBL5077144 214485 None 0 Human Binding pKi = 6.1 6.1 -575 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5092761 215388 None 0 Human Binding pKi = 6.1 6.1 -1258 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL428326 213438 None 0 Human Binding pKi = 8.0 8.0 -17 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
168295173 192311 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 192311 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44401285 135675 None 0 Human Binding pKi = 6.1 6.1 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 636 13 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL372966 135675 None 0 Human Binding pKi = 6.1 6.1 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 636 13 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44265496 97049 None 0 Human Binding pKi = 5.1 5.1 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 97049 None 0 Human Binding pKi = 5.1 5.1 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
10134057 88657 None 0 Human Binding pKi = 5.0 5.0 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235815 88657 None 0 Human Binding pKi = 5.0 5.0 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44453902 95434 None 0 Human Binding pKi = 5.0 5.0 -1 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 391 10 5 3 2.4 N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
CHEMBL257040 95434 None 0 Human Binding pKi = 5.0 5.0 -1 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 391 10 5 3 2.4 N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
168274920 190263 None 0 Human Binding pKi = 5.0 5.0 -83 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 190263 None 0 Human Binding pKi = 5.0 5.0 -83 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44434715 167508 None 0 Human Binding pKi = 5.0 5.0 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 593 10 2 3 7.8 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
CHEMBL429983 167508 None 0 Human Binding pKi = 5.0 5.0 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 593 10 2 3 7.8 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
44434781 89904 None 0 Human Binding pKi = 5.0 5.0 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 89904 None 0 Human Binding pKi = 5.0 5.0 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434758 88694 None 0 Human Binding pKi = 4.0 4.0 -100 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL236002 88694 None 0 Human Binding pKi = 4.0 4.0 -100 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
25132524 176758 None 0 Human Binding pKi = 6.0 6.0 -5 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 176758 None 0 Human Binding pKi = 6.0 6.0 -5 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44400662 125168 None 0 Human Binding pKi = 6.0 6.0 -478 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 13 3 6 4.5 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL364463 125168 None 0 Human Binding pKi = 6.0 6.0 -478 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 13 3 6 4.5 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434568 89176 None 0 Human Binding pKi = 6.0 6.0 -213 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236650 89176 None 0 Human Binding pKi = 6.0 6.0 -213 3
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434843 88700 None 0 Human Binding pKi = 5.0 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 88700 None 0 Human Binding pKi = 5.0 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
168285313 191401 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 191401 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL412495 212998 None 0 Human Binding pKi = 7.0 7.0 -79 3
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)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](CCC(=O)O)NC1=O 10.1021/jm0501432
168272615 190387 None 0 Human Binding pKi = 5.0 5.0 -87 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 190387 None 0 Human Binding pKi = 5.0 5.0 -87 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44434858 167251 None 0 Human Binding pKi = 4 4.0 -9 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL429269 167251 None 0 Human Binding pKi = 4 4.0 -9 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
11292 431 None 0 Human Binding pKd = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
70669253 431 None 0 Human Binding pKd = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
1321 1942 None 0 Human Binding pKd None 7.3 7.3 -15 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
1328 1943 None 0 Human Binding pKd None 8.3 8.3 -15 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9832440
1333 1763 None 0 Human Binding pKd None 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
166638272 1763 None 0 Human Binding pKd None 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
44134812 1763 None 0 Human Binding pKd None 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
None 216309 125I-NDP-MSH 0 Human Binding pKi = 7.9 7.9 -11 4
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
None 216309 125I-[Nle4,D-Phe7]Alpha-MSH 0 Human Binding pKi = 7.9 7.9 -11 4
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
3198 205513 None 76 Human Binding pKi = 8.4 8.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205513 None 76 Human Binding pKi = 8.4 8.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205513 None 76 Human Binding pKi = 8.4 8.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2726 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 None 68 Human Binding pKi = 8.3 8.3 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1016 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3747 None 78 Human Binding pKi = 8.3 8.3 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
4189 206922 None 96 Human Binding pKi = 8.3 8.3 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206922 None 96 Human Binding pKi = 8.3 8.3 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206922 None 96 Human Binding pKi = 8.3 8.3 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2247 505 None 81 Human Binding pKi = 8.3 8.3 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 None 81 Human Binding pKi = 8.3 8.3 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 None 81 Human Binding pKi = 8.3 8.3 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 None 81 Human Binding pKi = 8.3 8.3 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 None 81 Human Binding pKi = 8.3 8.3 -147 42
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
176 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157.0 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 None 66 Human Binding pKi = 8.3 8.3 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
134611880 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
16132265 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
16132265.0 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
3633 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
4931 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
CHEMBL1201610 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
DB01285 277 None 0 Human Binding pKi = 8.2 8.2 -5 5
NoneNone
Drug Central None None None None None
None 216310 125I-NDP-MSH 0 Human Binding pKi = 6.1 6.1 -7 4
NoneNone
PDSP KiDatabase 961 29 13 12 -1.5 CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N None
None 216310 125I-[Nle4,D-Phe7]Alpha-MSH 0 Human Binding pKi = 6.1 6.1 -7 4
NoneNone
PDSP KiDatabase 961 29 13 12 -1.5 CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N None
11993702 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
11993702.0 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
5416 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
9272 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
CHEMBL3301624 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
DB11700 3593 None 18 Human Binding pKi = 8.1 8.1 -3 5
NoneNone
Drug Central None None None None None
131839615 212636 None 26 Human Binding pKi = 8.1 8.1 -1 2
NoneNone
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
16133835 212636 None 26 Human Binding pKi = 8.1 8.1 -1 2
NoneNone
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
CHEMBL407070 212636 None 26 Human Binding pKi = 8.1 8.1 -1 2
NoneNone
Drug Central None None None 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)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(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 None
10408 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
5329 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
9941379 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
9941379.0 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
CHEMBL2070241 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
DB11653 720 None 28 Human Binding pKi = 7.3 7.3 -23 4
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
134611880 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
16132265 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
16132265.0 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
3633 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
4931 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
CHEMBL1201610 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
DB01285 277 None 0 Human Binding pKi = 7.1 7.1 -5 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
11993702 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
11993702.0 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
5416 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
9272 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
CHEMBL3301624 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
DB11700 3593 None 18 Human Binding pKi = 8 8.0 -3 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
1325 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
1325 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1325 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
6440621 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
6440621 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
6440621 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
9898183 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
9898183 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
9898183 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
CHEMBL3422426 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
CHEMBL3422426 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL3422426 3600 None 14 Human Binding pKi = 9 9.0 -5 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
1325 3600 None 14 Rat Binding pKi = 9.1 9.1 -12 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
6440621 3600 None 14 Rat Binding pKi = 9.1 9.1 -12 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
9898183 3600 None 14 Rat Binding pKi = 9.1 9.1 -12 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL3422426 3600 None 14 Rat Binding pKi = 9.1 9.1 -12 7
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1320 366 None 0 Human Binding pKi None 8.2 8.2 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
1320 366 None 0 Human Binding pKi None 8.2 8.2 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16162729 366 None 0 Human Binding pKi None 8.2 8.2 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
16162729 366 None 0 Human Binding pKi None 8.2 8.2 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1323 2688 None 55 Human Binding pKi None 8.3 8.3 -72 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
92432 2688 None 55 Human Binding pKi None 8.3 8.3 -72 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL430239 2688 None 55 Human Binding pKi None 8.3 8.3 -72 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1324 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16154396 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16197727 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16197727.0 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
44285019 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
57514683 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
91898441 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL441738 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
DB04931 302 None 25 Human Binding pKi None 8.9 8.9 -2 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100