Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
1323 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 2649 49 None -58 8 Human 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 211307 0 None -3 4 Human 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.2 pEC50 = 10.2 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
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 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16154396 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
44285019 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
57514683 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
91898441 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL441738 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
DB04931 299 23 None -7 9 Mouse 10.1 pEC50 = 10.1 Functional
Agonistic activity against mouse MC3RAgonistic activity against mouse MC3R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
1324 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 299 23 None -7 9 Mouse 10.0 pEC50 = 10.0 Functional
Effective concentration against mouse Melanocortin 3 receptorEffective concentration against mouse Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303608
1324 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 299 23 None -7 9 Mouse 10.0 pEC50 = 10 Functional
Functional activity at the mouse melanocortin 3 receptorFunctional activity at the mouse melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm010061n
1324 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 299 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
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 190352 0 None -2 4 Human 10.0 pEC50 = 10.0 Functional
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 190352 0 None -2 4 Human 10.0 pEC50 = 10.0 Functional
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 190363 0 None 10 3 Human 10.0 pEC50 = 10.0 Functional
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 190363 0 None 10 3 Human 10.0 pEC50 = 10.0 Functional
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 211768 0 None -5 4 Mouse 10.0 pEC50 = 10.0 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -16 9 Human 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 299 23 None -7 9 Mouse 9.9 pEC50 = 9.9 Functional
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 135922 0 None -3 4 Mouse 9.8 pEC50 = 9.8 Functional
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 135922 0 None -3 4 Mouse 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 3536 18 None 1 4 Human 9.8 pEC50 = 9.8 Functional
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 189492 0 None -1 4 Human 9.8 pEC50 = 9.8 Functional
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 189492 0 None -1 4 Human 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 81176 0 None -7 4 Mouse 9.8 pEC50 = 9.8 Functional
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 81176 0 None -7 4 Mouse 9.8 pEC50 = 9.8 Functional
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 210628 0 None -8 4 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.8 pEC50 = 9.8 Functional
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 2649 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
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 2649 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
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 2649 49 None -5 8 Mouse 9.7 pEC50 = 9.7 Functional
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 135922 0 None -3 4 Mouse 9.7 pEC50 = 9.7 Functional
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 135922 0 None -3 4 Mouse 9.7 pEC50 = 9.7 Functional
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 190718 0 None -4 4 Human 9.7 pEC50 = 9.7 Functional
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 190718 0 None -4 4 Human 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 299 23 None -7 9 Mouse 9.7 pEC50 = 9.7 Functional
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 211712 0 None -10 5 Human 9.7 pEC50 = 9.7 Functional
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 115739 0 None -2 4 Mouse 9.7 pEC50 = 9.7 Functional
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 115739 0 None -2 4 Mouse 9.7 pEC50 = 9.7 Functional
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 115742 0 None -4 4 Mouse 9.7 pEC50 = 9.7 Functional
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 115742 0 None -4 4 Mouse 9.7 pEC50 = 9.7 Functional
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 2649 49 None -58 8 Human 9.7 pEC50 = 9.7 Functional
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 2649 49 None -58 8 Human 9.7 pEC50 = 9.7 Functional
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 2649 49 None -58 8 Human 9.7 pEC50 = 9.7 Functional
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 115738 0 None -5 4 Mouse 9.7 pEC50 = 9.7 Functional
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 115738 0 None -5 4 Mouse 9.7 pEC50 = 9.7 Functional
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 208394 0 None -5 4 Mouse 9.7 pEC50 = 9.7 Functional
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 123465 0 None -8 5 Mouse 9.7 pEC50 = 9.7 Functional
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 123465 0 None -8 5 Mouse 9.7 pEC50 = 9.7 Functional
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 207534 31 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
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 207534 31 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
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 207534 31 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
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 207534 31 None -2 8 Mouse 9.7 pEC50 = 9.7 Functional
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 191028 0 None 1 4 Human 9.6 pEC50 = 9.6 Functional
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 191028 0 None 1 4 Human 9.6 pEC50 = 9.6 Functional
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 123465 0 None -8 5 Mouse 9.6 pEC50 = 9.6 Functional
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 123465 0 None -8 5 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 210794 0 None -2 5 Rat 9.6 pEC50 = 9.6 Functional
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 211418 0 None -4 5 Rat 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -7 9 Mouse 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 299 23 None -16 9 Human 9.6 pEC50 = 9.6 Functional
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 2649 49 None -58 8 Human 9.6 pEC50 = 9.6 Functional
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 2649 49 None -58 8 Human 9.6 pEC50 = 9.6 Functional
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 2649 49 None -58 8 Human 9.6 pEC50 = 9.6 Functional
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 208988 0 None -7 4 Mouse 9.6 pEC50 = 9.6 Functional
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 189839 0 None -2 4 Human 9.6 pEC50 = 9.6 Functional
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 189839 0 None -2 4 Human 9.6 pEC50 = 9.6 Functional
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 115737 0 None -2 4 Mouse 9.5 pEC50 = 9.5 Functional
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 115737 0 None -2 4 Mouse 9.5 pEC50 = 9.5 Functional
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 115745 0 None -4 4 Mouse 9.5 pEC50 = 9.5 Functional
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 115745 0 None -4 4 Mouse 9.5 pEC50 = 9.5 Functional
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 211091 0 None -7 4 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -16 9 Human 9.5 pEC50 = 9.5 Functional
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 189362 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
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 189362 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
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 189671 0 None -3 4 Human 9.5 pEC50 = 9.5 Functional
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 189671 0 None -3 4 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.5 pEC50 = 9.5 Functional
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 210806 15 None 22 7 Human 9.5 pEC50 = 9.5 Functional
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 210806 15 None 22 7 Human 9.5 pEC50 = 9.5 Functional
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 210806 15 None 22 7 Human 9.5 pEC50 = 9.5 Functional
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 210806 15 None 22 7 Human 9.5 pEC50 = 9.5 Functional
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 191568 0 None -3 4 Human 9.5 pEC50 = 9.5 Functional
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 191568 0 None -3 4 Human 9.5 pEC50 = 9.5 Functional
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 190786 0 None -1 4 Human 9.5 pEC50 = 9.5 Functional
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 190786 0 None -1 4 Human 9.5 pEC50 = 9.5 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 211352 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 299 23 None -16 9 Human 9.4 pEC50 = 9.4 Functional
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 208882 2 None -8 4 Mouse 9.4 pEC50 = 9.4 Functional
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 190328 0 None -1 4 Human 9.4 pEC50 = 9.4 Functional
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 190328 0 None -1 4 Human 9.4 pEC50 = 9.4 Functional
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 79541 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
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 79541 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
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 207534 31 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207534 31 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207534 31 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
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 207534 31 None -2 8 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 299 23 None -7 9 Mouse 9.4 pEC50 = 9.4 Functional
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 115735 0 None -8 4 Mouse 9.4 pEC50 = 9.4 Functional
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 115735 0 None -8 4 Mouse 9.4 pEC50 = 9.4 Functional
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 80779 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
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 80779 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 207534 31 None -2 8 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 168330 17 None 1 4 Mouse 9.3 pEC50 = 9.3 Functional
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 115743 0 None -4 4 Mouse 9.2 pEC50 = 9.2 Functional
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 115743 0 None -4 4 Mouse 9.2 pEC50 = 9.2 Functional
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 191807 0 None -6 4 Human 9.2 pEC50 = 9.2 Functional
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 191807 0 None -6 4 Human 9.2 pEC50 = 9.2 Functional
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 115744 0 None -4 4 Mouse 9.2 pEC50 = 9.2 Functional
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 115744 0 None -4 4 Mouse 9.2 pEC50 = 9.2 Functional
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 207534 31 None -7 8 Human 9.2 pEC50 = 9.2 Functional
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 207534 31 None -7 8 Human 9.2 pEC50 = 9.2 Functional
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 207534 31 None -7 8 Human 9.2 pEC50 = 9.2 Functional
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 207534 31 None -7 8 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 712 26 None -5 4 Human 9.2 pEC50 = 9.2 Functional
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 210957 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
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 190645 0 None -1 4 Human 9.2 pEC50 = 9.2 Functional
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 190645 0 None -1 4 Human 9.2 pEC50 = 9.2 Functional
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 155330 0 None -2 4 Human 9.2 pEC50 = 9.2 Functional
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 155330 0 None -2 4 Human 9.2 pEC50 = 9.2 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 207534 31 None -2 8 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -16 9 Human 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 299 23 None -7 9 Mouse 9.1 pEC50 = 9.1 Functional
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 115733 0 None -10 4 Mouse 9.1 pEC50 = 9.1 Functional
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 115733 0 None -10 4 Mouse 9.1 pEC50 = 9.1 Functional
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 115730 0 None -7 4 Mouse 9.0 pEC50 = 9.0 Functional
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 115730 0 None -7 4 Mouse 9.0 pEC50 = 9.0 Functional
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 189894 0 None -3 4 Human 9.0 pEC50 = 9.0 Functional
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 189894 0 None -3 4 Human 9.0 pEC50 = 9.0 Functional
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 207882 0 None -4 4 Mouse 9.0 pEC50 = 9 Functional
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 138740 0 None -5 3 Human 9.0 pEC50 = 9 Functional
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 138740 0 None -5 3 Human 9.0 pEC50 = 9 Functional
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 163568 0 None 3 3 Human 9.0 pEC50 = 9 Functional
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 163568 0 None 3 3 Human 9.0 pEC50 = 9 Functional
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 208555 0 None -5 3 Mouse 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 207534 31 None -7 8 Human 9.0 pEC50 = 9.0 Functional
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 211724 0 None -26 5 Human 9.0 pEC50 = 9.0 Functional
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 213511 0 None -12 4 Human 8.9 pEC50 = 8.9 Functional
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 208845 0 None 5 4 Human 8.9 pEC50 = 8.9 Functional
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 213349 0 None 4 3 Human 8.9 pEC50 = 8.9 Functional
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 137940 0 None -28 3 Human 8.9 pEC50 = 8.9 Functional
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 137940 0 None -28 3 Human 8.9 pEC50 = 8.9 Functional
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 115734 0 None -10 4 Mouse 8.9 pEC50 = 8.9 Functional
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 115734 0 None -10 4 Mouse 8.9 pEC50 = 8.9 Functional
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 207534 31 None -7 8 Human 8.9 pEC50 = 8.9 Functional
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 207534 31 None -7 8 Human 8.9 pEC50 = 8.9 Functional
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 207534 31 None -7 8 Human 8.9 pEC50 = 8.9 Functional
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 207534 31 None -7 8 Human 8.9 pEC50 = 8.9 Functional
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 213097 0 None -25 4 Human 8.8 pEC50 = 8.8 Functional
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 210076 0 None 2 4 Human 8.8 pEC50 = 8.8 Functional
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 2649 49 None -58 8 Human 8.8 pEC50 = 8.8 Functional
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 2649 49 None -58 8 Human 8.8 pEC50 = 8.8 Functional
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 2649 49 None -58 8 Human 8.8 pEC50 = 8.8 Functional
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 115731 0 None -8 4 Mouse 8.8 pEC50 = 8.8 Functional
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 115731 0 None -8 4 Mouse 8.8 pEC50 = 8.8 Functional
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 212100 0 None 5 3 Human 8.8 pEC50 = 8.8 Functional
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 211996 0 None 21 3 Human 8.8 pEC50 = 8.8 Functional
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 208992 0 None -5 2 Human 8.8 pEC50 = 8.8 Functional
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 207091 0 None -8 4 Mouse 8.8 pEC50 = 8.8 Functional
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 164081 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
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 164081 0 None 2 4 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 210715 0 None -6 4 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 164105 0 None 11 4 Human 8.7 pEC50 = 8.7 Functional
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 164105 0 None 11 4 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 2649 49 None -58 8 Human 8.7 pEC50 = 8.7 Functional
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 210469 1 None 25 4 Human 8.7 pEC50 = 8.7 Functional
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 115741 0 None -2 4 Mouse 8.7 pEC50 = 8.7 Functional
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 115741 0 None -2 4 Mouse 8.7 pEC50 = 8.7 Functional
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 209822 0 None -7 4 Mouse 8.7 pEC50 = 8.7 Functional
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 140914 0 None -19 3 Human 8.0 pEC50 = 8 Functional
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 140914 0 None -19 3 Human 8.0 pEC50 = 8 Functional
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 77596 0 None -2 3 Human 8.0 pEC50 = 8 Functional
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 77596 0 None -2 3 Human 8.0 pEC50 = 8 Functional
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 173305 0 None -25 4 Mouse 8.0 pEC50 = 8 Functional
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 173305 0 None -25 4 Mouse 8.0 pEC50 = 8 Functional
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 139219 0 None -60 5 Mouse 8.0 pEC50 = 8 Functional
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 139219 0 None -60 5 Mouse 8.0 pEC50 = 8 Functional
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 139219 0 None -60 5 Mouse 8.0 pEC50 = 8 Functional
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 207534 31 None -2 8 Mouse 8.0 pEC50 = 8.0 Functional
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 207534 31 None -2 8 Mouse 8.0 pEC50 = 8.0 Functional
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 207534 31 None -2 8 Mouse 8.0 pEC50 = 8.0 Functional
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 207534 31 None -2 8 Mouse 8.0 pEC50 = 8.0 Functional
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 154365 0 None 1 3 Human 7.0 pEC50 = 7 Functional
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 154365 0 None 1 3 Human 7.0 pEC50 = 7 Functional
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 175003 0 None -3 4 Mouse 7.0 pEC50 = 7 Functional
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 175003 0 None -3 4 Mouse 7.0 pEC50 = 7 Functional
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 175393 0 None -21 4 Mouse 7.0 pEC50 = 7 Functional
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 175393 0 None -21 4 Mouse 7.0 pEC50 = 7 Functional
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 209480 0 None -1 4 Mouse 7.0 pEC50 = 7 Functional
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 156437 0 None -38 3 Human 6.0 pEC50 = 6 Functional
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 156437 0 None -38 3 Human 6.0 pEC50 = 6 Functional
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 158672 0 None -1071 4 Human 6.0 pEC50 = 6 Functional
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 158672 0 None -1071 4 Human 6.0 pEC50 = 6 Functional
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 211132 0 None -4 4 Human 6.0 pEC50 = 6 Functional
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 175161 0 None -33 3 Mouse 5.0 pEC50 = 5 Functional
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 175161 0 None -33 3 Mouse 5.0 pEC50 = 5 Functional
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 201397 0 None -5 4 Mouse 4.0 pEC50 = 4 Functional
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 201397 0 None -5 4 Mouse 4.0 pEC50 = 4 Functional
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 201646 0 None -4 4 Mouse 4.0 pEC50 = 4 Functional
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 201646 0 None -4 4 Mouse 4.0 pEC50 = 4 Functional
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 93693 0 None -93 3 Human 6.0 pEC50 = 6 Functional
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 93693 0 None -93 3 Human 6.0 pEC50 = 6 Functional
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 66719 0 None -70 3 Human 6.0 pEC50 = 6.0 Functional
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 66719 0 None -70 3 Human 6.0 pEC50 = 6.0 Functional
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 123455 0 None -26 3 Human 6.0 pEC50 = 6.0 Functional
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 123455 0 None -26 3 Human 6.0 pEC50 = 6.0 Functional
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 69931 0 None -36 4 Mouse 7.0 pEC50 = 7.0 Functional
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 69931 0 None -36 4 Mouse 7.0 pEC50 = 7.0 Functional
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 172042 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
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 172042 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
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 207772 0 None -9 4 Mouse 5.0 pEC50 = 5.0 Functional
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 173925 0 None -3 4 Mouse 7.0 pEC50 = 7.0 Functional
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 173925 0 None -3 4 Mouse 7.0 pEC50 = 7.0 Functional
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 211846 0 None -3 4 Mouse 7.0 pEC50 = 7.0 Functional
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 7946 0 None -173 4 Human 5.0 pEC50 = 5.0 Functional
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 7946 0 None -173 4 Human 5.0 pEC50 = 5.0 Functional
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 78169 0 None -26 4 Mouse 5.0 pEC50 = 5.0 Functional
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 78169 0 None -26 4 Mouse 5.0 pEC50 = 5.0 Functional
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 188262 0 None -83 3 Human 7.0 pEC50 = 7.0 Functional
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 188262 0 None -83 3 Human 7.0 pEC50 = 7.0 Functional
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 121919 0 None -2 4 Human 8.0 pEC50 = 8.0 Functional
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 121919 0 None -2 4 Human 8.0 pEC50 = 8.0 Functional
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 182577 0 None -47 3 Mouse 8.0 pEC50 = 8.0 Functional
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 182577 0 None -47 3 Mouse 8.0 pEC50 = 8.0 Functional
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 208364 0 None -2 4 Human 8.0 pEC50 = 8.0 Functional
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 209659 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
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 213525 0 None -102 4 Human 8.0 pEC50 = 8.0 Functional
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 111251 0 None -26 5 Mouse 7.9 pEC50 = 7.9 Functional
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 111251 0 None -26 5 Mouse 7.9 pEC50 = 7.9 Functional
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 173976 0 None -363 4 Mouse 7.0 pEC50 = 7.0 Functional
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 173976 0 None -363 4 Mouse 7.0 pEC50 = 7.0 Functional
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 180914 0 None -2 3 Mouse 7.0 pEC50 = 7.0 Functional
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 180914 0 None -2 3 Mouse 7.0 pEC50 = 7.0 Functional
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 180953 0 None -3 3 Mouse 7.0 pEC50 = 7.0 Functional
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 180953 0 None -3 3 Mouse 7.0 pEC50 = 7.0 Functional
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 173012 0 None -29 3 Human 6.0 pEC50 = 6.0 Functional
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 173012 0 None -29 3 Human 6.0 pEC50 = 6.0 Functional
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 157535 0 None -12 3 Mouse 6.0 pEC50 = 6.0 Functional
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 157535 0 None -12 3 Mouse 6.0 pEC50 = 6.0 Functional
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 173370 0 None -52 4 Mouse 6.0 pEC50 = 6.0 Functional
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 173370 0 None -52 4 Mouse 6.0 pEC50 = 6.0 Functional
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 78571 0 None -19 4 Human 6.0 pEC50 = 6.0 Functional
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 78571 0 None -19 4 Human 6.0 pEC50 = 6.0 Functional
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 177895 0 None -37 3 Human 7.0 pEC50 = 7.0 Functional
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 177895 0 None -37 3 Human 7.0 pEC50 = 7.0 Functional
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 210079 0 None -24 4 Human 6.0 pEC50 = 6.0 Functional
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 79818 0 None -125 3 Human 6.0 pEC50 = 6.0 Functional
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 79818 0 None -125 3 Human 6.0 pEC50 = 6.0 Functional
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 93865 0 None -69 3 Human 6.9 pEC50 = 6.9 Functional
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 93865 0 None -69 3 Human 6.9 pEC50 = 6.9 Functional
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 166727 0 None -6 4 Human 6.9 pEC50 = 6.9 Functional
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 166727 0 None -6 4 Human 6.9 pEC50 = 6.9 Functional
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 7878 18 None -95 4 Human 5.9 pEC50 = 5.9 Functional
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 7878 18 None -95 4 Human 5.9 pEC50 = 5.9 Functional
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 7878 18 None -95 4 Human 5.9 pEC50 = 5.9 Functional
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 8035 0 None -165 4 Human 4.9 pEC50 = 4.9 Functional
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 8035 0 None -165 4 Human 4.9 pEC50 = 4.9 Functional
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 138984 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
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 138984 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
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 214023 0 None -169 4 Mouse 4.9 pEC50 = 4.9 Functional
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 171200 0 None -15 3 Human 7.9 pEC50 = 7.9 Functional
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 171200 0 None -15 3 Human 7.9 pEC50 = 7.9 Functional
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 163810 0 None -1 4 Human 7.9 pEC50 = 7.9 Functional
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 163810 0 None -1 4 Human 7.9 pEC50 = 7.9 Functional
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 209659 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
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 208225 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
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 165943 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
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 165943 0 None -2 4 Human 6.9 pEC50 = 6.9 Functional
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 204489 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
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 204489 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
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 168313 0 None -107 4 Human 5.9 pEC50 = 5.9 Functional
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 168313 0 None -107 4 Human 5.9 pEC50 = 5.9 Functional
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 207534 31 None -2 8 Mouse 5.9 pEC50 = 5.9 Functional
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 207534 31 None -2 8 Mouse 5.9 pEC50 = 5.9 Functional
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 207534 31 None -2 8 Mouse 5.9 pEC50 = 5.9 Functional
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 207534 31 None -2 8 Mouse 5.9 pEC50 = 5.9 Functional
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 137068 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
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 137068 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
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 155369 0 None -30 3 Human 6.9 pEC50 = 6.9 Functional
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 155369 0 None -30 3 Human 6.9 pEC50 = 6.9 Functional
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 213811 0 None -141 4 Mouse 5.9 pEC50 = 5.9 Functional
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 206724 0 None -30 4 Mouse 4.9 pEC50 = 4.9 Functional
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 208863 1 None -35 8 Mouse 6.9 pEC50 = 6.9 Functional
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 97515 0 None -630 5 Mouse 5.9 pEC50 = 5.9 Functional
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 97515 0 None -630 5 Mouse 5.9 pEC50 = 5.9 Functional
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 213683 0 None -169 4 Human 6.9 pEC50 = 6.9 Functional
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 207753 0 None 1 4 Human 7.9 pEC50 = 7.9 Functional
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 106529 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
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 106529 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
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 210073 0 None 1 4 Human 7.9 pEC50 = 7.9 Functional
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 212657 0 None -8 4 Human 7.9 pEC50 = 7.9 Functional
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 212370 0 None -37 4 Human 6.9 pEC50 = 6.9 Functional
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 105617 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
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 105617 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
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 175474 0 None -4 4 Mouse 5.9 pEC50 = 5.9 Functional
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 175474 0 None -4 4 Mouse 5.9 pEC50 = 5.9 Functional
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 156545 0 None -29 3 Mouse 4.9 pEC50 = 4.9 Functional
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 156545 0 None -29 3 Mouse 4.9 pEC50 = 4.9 Functional
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 3747 37 None -467 7 Rat 5.9 pEC50 = 5.9 Functional
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 3747 37 None -467 7 Rat 5.9 pEC50 = 5.9 Functional
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 3747 37 None -467 7 Rat 5.9 pEC50 = 5.9 Functional
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 69050 0 None -64 4 Mouse 6.9 pEC50 = 6.9 Functional
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 69050 0 None -64 4 Mouse 6.9 pEC50 = 6.9 Functional
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 126717 0 None -8 3 Human 5.9 pEC50 = 5.9 Functional
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 126717 0 None -8 3 Human 5.9 pEC50 = 5.9 Functional
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 207632 0 None -74 3 Human 6.9 pEC50 = 6.9 Functional
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 209724 0 None -1 4 Mouse 4.9 pEC50 = 4.9 Functional
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 79584 0 None -5 3 Human 5.9 pEC50 = 5.9 Functional
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 79584 0 None -5 3 Human 5.9 pEC50 = 5.9 Functional
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 67278 0 None -147 4 Mouse 6.9 pEC50 = 6.9 Functional
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 67278 0 None -147 4 Mouse 6.9 pEC50 = 6.9 Functional
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 212353 0 None -1 4 Human 7.9 pEC50 = 7.9 Functional
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 179520 0 None -23 3 Mouse 7.9 pEC50 = 7.9 Functional
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 179520 0 None -23 3 Mouse 7.9 pEC50 = 7.9 Functional
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 180944 0 None -2 4 Mouse 7.9 pEC50 = 7.9 Functional
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 180944 0 None -2 4 Mouse 7.9 pEC50 = 7.9 Functional
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 182508 0 None -35 3 Mouse 7.9 pEC50 = 7.9 Functional
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 182508 0 None -35 3 Mouse 7.9 pEC50 = 7.9 Functional
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 123562 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
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 123562 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
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 207464 0 None -21 4 Human 6.9 pEC50 = 6.9 Functional
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 122044 0 None -69 4 Human 5.9 pEC50 = 5.9 Functional
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 122044 0 None -69 4 Human 5.9 pEC50 = 5.9 Functional
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 168289 0 None -446 4 Human 5.9 pEC50 = 5.9 Functional
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 168289 0 None -446 4 Human 5.9 pEC50 = 5.9 Functional
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 172680 0 None -10 3 Mouse 5.9 pEC50 = 5.9 Functional
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 172680 0 None -10 3 Mouse 5.9 pEC50 = 5.9 Functional
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 3747 37 None -239 7 Human 5.9 pEC50 = 5.9 Functional
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 3747 37 None -239 7 Human 5.9 pEC50 = 5.9 Functional
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 3747 37 None -239 7 Human 5.9 pEC50 = 5.9 Functional
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 155758 0 None -10 6 Mouse 4.9 pEC50 = 4.9 Functional
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 155758 0 None -10 6 Mouse 4.9 pEC50 = 4.9 Functional
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 155496 0 None -1 4 Mouse 4.9 pEC50 = 4.9 Functional
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 155496 0 None -1 4 Mouse 4.9 pEC50 = 4.9 Functional
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 181983 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 181983 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 80686 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
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 80686 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
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 126942 0 None -12 3 Human 5.8 pEC50 = 5.8 Functional
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 126942 0 None -12 3 Human 5.8 pEC50 = 5.8 Functional
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 121831 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
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 121831 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
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 156149 0 None -81 4 Mouse 5.8 pEC50 = 5.8 Functional
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 156149 0 None -81 4 Mouse 5.8 pEC50 = 5.8 Functional
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 176445 0 None -12 3 Human 6.8 pEC50 = 6.8 Functional
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 176445 0 None -12 3 Human 6.8 pEC50 = 6.8 Functional
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 79819 0 None -77 3 Human 5.8 pEC50 = 5.8 Functional
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 79819 0 None -77 3 Human 5.8 pEC50 = 5.8 Functional
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 159170 0 None -26 4 Human 5.8 pEC50 = 5.8 Functional
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 159170 0 None -26 4 Human 5.8 pEC50 = 5.8 Functional
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 176356 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 176356 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 207308 0 None -11 3 Human 5.8 pEC50 = 5.8 Functional
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 176150 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
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 176150 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
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 138988 0 None -50 3 Human 7.8 pEC50 = 7.8 Functional
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 138988 0 None -50 3 Human 7.8 pEC50 = 7.8 Functional
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 173765 0 None -9 4 Mouse 7.8 pEC50 = 7.8 Functional
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 173765 0 None -9 4 Mouse 7.8 pEC50 = 7.8 Functional
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 209235 0 None -36 4 Mouse 7.8 pEC50 = 7.8 Functional
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 213345 0 None -12 4 Human 7.8 pEC50 = 7.8 Functional
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 172305 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 172305 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 181608 0 None -4 3 Mouse 6.8 pEC50 = 6.8 Functional
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 181608 0 None -4 3 Mouse 6.8 pEC50 = 6.8 Functional
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 12851 0 None -61 3 Human 6.8 pEC50 = 6.8 Functional
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 12851 0 None -61 3 Human 6.8 pEC50 = 6.8 Functional
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 12851 0 None -61 3 Human 6.8 pEC50 = 6.8 Functional
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 208223 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
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 159009 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
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 159009 0 None -3 3 Mouse 5.8 pEC50 = 5.8 Functional
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 212348 2 None -138 7 Mouse 5.8 pEC50 = 5.8 Functional
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 209659 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
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 209480 0 None -1 4 Mouse 4.8 pEC50 = 4.8 Functional
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 182619 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 182619 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 96391 0 None -154 4 Mouse 6.8 pEC50 = 6.8 Functional
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 96391 0 None -154 4 Mouse 6.8 pEC50 = 6.8 Functional
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 182619 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 182619 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 208863 1 None -35 8 Mouse 6.8 pEC50 = 6.8 Functional
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 95155 0 None -93 3 Human 6.8 pEC50 = 6.8 Functional
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 95155 0 None -93 3 Human 6.8 pEC50 = 6.8 Functional
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 210072 0 None -2 4 Human 7.8 pEC50 = 7.8 Functional
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 157307 0 None -181 4 Mouse 7.8 pEC50 = 7.8 Functional
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 157307 0 None -181 4 Mouse 7.8 pEC50 = 7.8 Functional
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 212714 0 None -38 4 Human 7.8 pEC50 = 7.8 Functional
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 207534 31 None -7 8 Human 7.8 pEC50 = 7.8 Functional
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 207534 31 None -7 8 Human 7.8 pEC50 = 7.8 Functional
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 207534 31 None -7 8 Human 7.8 pEC50 = 7.8 Functional
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 207534 31 None -7 8 Human 7.8 pEC50 = 7.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 155384 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
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 155384 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
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 3747 37 None -239 7 Human 6.8 pEC50 = 6.8 Functional
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 3747 37 None -239 7 Human 6.8 pEC50 = 6.8 Functional
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 3747 37 None -239 7 Human 6.8 pEC50 = 6.8 Functional
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 156261 0 None -7 4 Mouse 6.8 pEC50 = 6.8 Functional
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 156261 0 None -7 4 Mouse 6.8 pEC50 = 6.8 Functional
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 208863 1 None -35 8 Mouse 6.8 pEC50 = 6.8 Functional
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 204820 0 None -19 3 Human 6.8 pEC50 = 6.8 Functional
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 204820 0 None -19 3 Human 6.8 pEC50 = 6.8 Functional
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 164719 0 None -112 2 Human 5.8 pEC50 = 5.8 Functional
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 164719 0 None -112 2 Human 5.8 pEC50 = 5.8 Functional
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 174598 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
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 174598 0 None -14 3 Mouse 4.8 pEC50 = 4.8 Functional
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 207305 0 None -3 3 Human 5.8 pEC50 = 5.8 Functional
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 209733 0 None -281 4 Human 6.8 pEC50 = 6.8 Functional
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 158832 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
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 158832 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
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 121912 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
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 121912 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
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 189793 0 None -31 4 Human 6.8 pEC50 = 6.8 Functional
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 189793 0 None -31 4 Human 6.8 pEC50 = 6.8 Functional
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 80906 0 None -102 3 Human 6.8 pEC50 = 6.8 Functional
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 80906 0 None -102 3 Human 6.8 pEC50 = 6.8 Functional
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 167774 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
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 167774 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
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 212346 0 None -74 4 Mouse 4.8 pEC50 = 4.8 Functional
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 210175 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
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 207358 0 None -53 4 Mouse 6.8 pEC50 = 6.8 Functional
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 195425 0 None -33 4 Mouse 4.8 pEC50 = 4.8 Functional
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 195425 0 None -33 4 Mouse 4.8 pEC50 = 4.8 Functional
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 181714 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 181714 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 2649 49 None -58 8 Human 7.8 pEC50 = 7.8 Functional
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 167515 0 None -33 3 Human 7.8 pEC50 = 7.8 Functional
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 167515 0 None -33 3 Human 7.8 pEC50 = 7.8 Functional
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 212623 0 None -125 4 Human 7.8 pEC50 = 7.8 Functional
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 65980 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
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 65980 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
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 207303 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
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 212348 2 None -15 7 Human 6.8 pEC50 = 6.8 Functional
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 207416 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
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 208226 0 None -63 4 Human 5.8 pEC50 = 5.8 Functional
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 8308 3 None -257 7 Mouse 5.8 pEC50 = 5.8 Functional
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 8308 3 None -257 7 Mouse 5.8 pEC50 = 5.8 Functional
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 201106 0 None 1 4 Mouse 5.8 pEC50 = 5.8 Functional
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 201106 0 None 1 4 Mouse 5.8 pEC50 = 5.8 Functional
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 208226 0 None -63 4 Human 5.8 pEC50 = 5.8 Functional
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 208863 1 None -35 8 Mouse 6.8 pEC50 = 6.8 Functional
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 181714 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 181714 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
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 209169 0 None -5 5 Mouse 5.8 pEC50 = 5.8 Functional
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 210087 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
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 79352 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
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 79352 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
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 121922 0 None 2 4 Human 5.8 pEC50 = 5.8 Functional
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 121922 0 None 2 4 Human 5.8 pEC50 = 5.8 Functional
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 213613 0 None -281 4 Human 7.7 pEC50 = 7.7 Functional
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 207767 0 None -12 4 Mouse 6.8 pEC50 = 6.8 Functional
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 14862 0 None -158 4 Human 5.8 pEC50 = 5.8 Functional
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 14862 0 None -158 4 Human 5.8 pEC50 = 5.8 Functional
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 119469 0 None -251 2 Human 5.8 pEC50 = 5.8 Functional
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 119469 0 None -251 2 Human 5.8 pEC50 = 5.8 Functional
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 172221 0 None -10 3 Mouse 4.8 pEC50 = 4.8 Functional
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 172221 0 None -10 3 Mouse 4.8 pEC50 = 4.8 Functional
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 121920 0 None -3 4 Human 5.7 pEC50 = 5.7 Functional
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 121920 0 None -3 4 Human 5.7 pEC50 = 5.7 Functional
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 207780 0 None -120 4 Mouse 5.7 pEC50 = 5.7 Functional
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 163411 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
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 163411 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
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 209564 0 None -7 5 Mouse 7.7 pEC50 = 7.7 Functional
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 212011 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
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 156217 0 None -11 3 Human 7.7 pEC50 = 7.7 Functional
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 156217 0 None -11 3 Human 7.7 pEC50 = 7.7 Functional
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 213503 0 None -18 4 Human 7.7 pEC50 = 7.7 Functional
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 207774 0 None -25 4 Mouse 6.7 pEC50 = 6.7 Functional
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 190116 0 None -39 4 Human 6.7 pEC50 = 6.7 Functional
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 190116 0 None -39 4 Human 6.7 pEC50 = 6.7 Functional
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 207771 0 None -60 4 Mouse 5.7 pEC50 = 5.7 Functional
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 173940 0 None -147 3 Mouse 4.7 pEC50 = 4.7 Functional
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 173940 0 None -147 3 Mouse 4.7 pEC50 = 4.7 Functional
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 189669 0 None -66 4 Human 6.7 pEC50 = 6.7 Functional
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 189669 0 None -66 4 Human 6.7 pEC50 = 6.7 Functional
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 208863 1 None -35 8 Mouse 6.7 pEC50 = 6.7 Functional
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 210080 0 None -2 4 Human 5.7 pEC50 = 5.7 Functional
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 195666 0 None -25 4 Mouse 4.7 pEC50 = 4.7 Functional
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 195666 0 None -25 4 Mouse 4.7 pEC50 = 4.7 Functional
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 141056 0 None 4 3 Human 8.7 pEC50 = 8.7 Functional
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 141056 0 None 4 3 Human 8.7 pEC50 = 8.7 Functional
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 212392 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
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 188149 0 None -3 4 Human 8.7 pEC50 = 8.7 Functional
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 188149 0 None -3 4 Human 8.7 pEC50 = 8.7 Functional
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 207091 0 None -8 4 Mouse 8.7 pEC50 = 8.7 Functional
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 212172 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
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 209659 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
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 207534 31 None -2 8 Mouse 8.7 pEC50 = 8.7 Functional
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 207534 31 None -2 8 Mouse 8.7 pEC50 = 8.7 Functional
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 207534 31 None -2 8 Mouse 8.7 pEC50 = 8.7 Functional
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 207534 31 None -2 8 Mouse 8.7 pEC50 = 8.7 Functional
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 213346 0 None -2 3 Human 8.7 pEC50 = 8.7 Functional
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 209821 0 None -4 4 Mouse 8.7 pEC50 = 8.7 Functional
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 115019 0 None -10 4 Mouse 8.6 pEC50 = 8.6 Functional
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 115019 0 None -10 4 Mouse 8.6 pEC50 = 8.6 Functional
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 712 26 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 712 26 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 712 26 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 712 26 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 712 26 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 2649 49 None -58 8 Human 8.6 pEC50 = 8.6 Functional
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 2649 49 None -58 8 Human 8.6 pEC50 = 8.6 Functional
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 2649 49 None -58 8 Human 8.6 pEC50 = 8.6 Functional
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 209823 0 None -7 3 Mouse 8.6 pEC50 = 8.6 Functional
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 190521 0 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 190521 0 None -5 4 Human 8.6 pEC50 = 8.6 Functional
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 207534 31 None -7 8 Human 8.6 pEC50 = 8.6 Functional
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 207534 31 None -7 8 Human 8.6 pEC50 = 8.6 Functional
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 207534 31 None -7 8 Human 8.6 pEC50 = 8.6 Functional
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 207534 31 None -7 8 Human 8.6 pEC50 = 8.6 Functional
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 159649 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
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 159649 0 None 2 3 Human 8.6 pEC50 = 8.6 Functional
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 208938 0 None -83 6 Human 8.6 pEC50 = 8.6 Functional
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 211847 0 None -66 4 Mouse 7.7 pEC50 = 7.7 Functional
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 158900 0 None -13 4 Human 7.7 pEC50 = 7.7 Functional
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 158900 0 None -13 4 Human 7.7 pEC50 = 7.7 Functional
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 207766 0 None -32 4 Mouse 6.7 pEC50 = 6.7 Functional
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 118297 0 None -53 4 Human 5.7 pEC50 = 5.7 Functional
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 118297 0 None -53 4 Human 5.7 pEC50 = 5.7 Functional
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 14861 0 None -112 4 Human 5.7 pEC50 = 5.7 Functional
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 14861 0 None -112 4 Human 5.7 pEC50 = 5.7 Functional
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 173158 0 None -25 4 Mouse 5.7 pEC50 = 5.7 Functional
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 173158 0 None -25 4 Mouse 5.7 pEC50 = 5.7 Functional
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 185921 0 None 3 3 Mouse 5.7 pEC50 = 5.7 Functional
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 185921 0 None 3 3 Mouse 5.7 pEC50 = 5.7 Functional
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 116449 0 None -25 2 Human 5.7 pEC50 = 5.7 Functional
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 116449 0 None -25 2 Human 5.7 pEC50 = 5.7 Functional
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 74085 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
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 74085 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
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 79473 0 None -141 3 Human 4.7 pEC50 = 4.7 Functional
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 79473 0 None -141 3 Human 4.7 pEC50 = 4.7 Functional
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 141424 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
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 141424 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
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 74085 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
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 74085 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
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 77711 0 None -38 3 Human 4.7 pEC50 = 4.7 Functional
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 77711 0 None -38 3 Human 4.7 pEC50 = 4.7 Functional
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 79657 0 None -11 3 Human 4.7 pEC50 = 4.7 Functional
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 79657 0 None -11 3 Human 4.7 pEC50 = 4.7 Functional
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 79820 0 None -44 3 Human 4.7 pEC50 = 4.7 Functional
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 79820 0 None -44 3 Human 4.7 pEC50 = 4.7 Functional
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 138486 0 None -50 3 Human 4.7 pEC50 = 4.7 Functional
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 138486 0 None -50 3 Human 4.7 pEC50 = 4.7 Functional
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 141424 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
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 141424 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
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 123522 0 None -4 3 Human 6.7 pEC50 = 6.7 Functional
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 123522 0 None -4 3 Human 6.7 pEC50 = 6.7 Functional
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 155985 0 None -50 4 Human 6.7 pEC50 = 6.7 Functional
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 155985 0 None -50 4 Human 6.7 pEC50 = 6.7 Functional
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 209478 0 None -177 4 Mouse 5.7 pEC50 = 5.7 Functional
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 97163 0 None -204 5 Mouse 4.7 pEC50 = 4.7 Functional
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 97163 0 None -204 5 Mouse 4.7 pEC50 = 4.7 Functional
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 195763 0 None -245 4 Mouse 4.7 pEC50 = 4.7 Functional
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 195763 0 None -245 4 Mouse 4.7 pEC50 = 4.7 Functional
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 79643 0 None -7 3 Human 5.7 pEC50 = 5.7 Functional
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 79643 0 None -7 3 Human 5.7 pEC50 = 5.7 Functional
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 122642 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
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 122642 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
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 174719 0 None -69 4 Mouse 7.7 pEC50 = 7.7 Functional
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 174719 0 None -69 4 Mouse 7.7 pEC50 = 7.7 Functional
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 209565 0 None -4 5 Mouse 7.7 pEC50 = 7.7 Functional
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 174464 0 None -11 4 Mouse 6.7 pEC50 = 6.7 Functional
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 174464 0 None -11 4 Mouse 6.7 pEC50 = 6.7 Functional
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 175136 0 None -104 4 Mouse 6.7 pEC50 = 6.7 Functional
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 175136 0 None -104 4 Mouse 6.7 pEC50 = 6.7 Functional
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 185318 0 None -1 4 Mouse 6.7 pEC50 = 6.7 Functional
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 185318 0 None -1 4 Mouse 6.7 pEC50 = 6.7 Functional
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 211609 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
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 158282 0 None -51 4 Human 5.7 pEC50 = 5.7 Functional
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 158282 0 None -51 4 Human 5.7 pEC50 = 5.7 Functional
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 138763 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
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 138763 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
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 172033 0 None -42 3 Human 6.7 pEC50 = 6.7 Functional
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 172033 0 None -42 3 Human 6.7 pEC50 = 6.7 Functional
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 182508 0 None -35 3 Mouse 7.7 pEC50 = 7.7 Functional
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 182508 0 None -35 3 Mouse 7.7 pEC50 = 7.7 Functional
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 111253 0 None -7 5 Mouse 7.7 pEC50 = 7.7 Functional
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 111253 0 None -7 5 Mouse 7.7 pEC50 = 7.7 Functional
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 139463 0 None -123 5 Mouse 7.6 pEC50 = 7.6 Functional
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 139463 0 None -123 5 Mouse 7.6 pEC50 = 7.6 Functional
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 183972 0 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
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 183972 0 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
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 132606 0 None -380 4 Mouse 6.7 pEC50 = 6.7 Functional
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 132606 0 None -380 4 Mouse 6.7 pEC50 = 6.7 Functional
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 155758 0 None -15 6 Human 4.7 pEC50 = 4.7 Functional
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 155758 0 None -15 6 Human 4.7 pEC50 = 4.7 Functional
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 207765 0 None -28 4 Mouse 5.7 pEC50 = 5.7 Functional
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 207848 0 None -6 4 Mouse 4.7 pEC50 = 4.7 Functional
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 212945 0 None -29 4 Human 7.6 pEC50 = 7.6 Functional
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 97392 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
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 97392 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
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 207768 0 None -11 4 Mouse 6.6 pEC50 = 6.6 Functional
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 93697 0 None -28 3 Human 6.6 pEC50 = 6.6 Functional
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 93697 0 None -28 3 Human 6.6 pEC50 = 6.6 Functional
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 110945 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
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 110945 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
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 159124 0 None 1 3 Mouse 5.6 pEC50 = 5.6 Functional
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 159124 0 None 1 3 Mouse 5.6 pEC50 = 5.6 Functional
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 79948 0 None -23 3 Human 6.6 pEC50 = 6.6 Functional
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 79948 0 None -23 3 Human 6.6 pEC50 = 6.6 Functional
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 97123 0 None -5 3 Mouse 4.6 pEC50 = 4.6 Functional
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 97123 0 None -5 3 Mouse 4.6 pEC50 = 4.6 Functional
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 65453 0 None -14 3 Human 5.6 pEC50 = 5.6 Functional
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 65453 0 None -14 3 Human 5.6 pEC50 = 5.6 Functional
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 176184 0 None -7 3 Human 6.6 pEC50 = 6.6 Functional
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 176184 0 None -7 3 Human 6.6 pEC50 = 6.6 Functional
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 121921 0 None -3 4 Human 5.6 pEC50 = 5.6 Functional
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 121921 0 None -3 4 Human 5.6 pEC50 = 5.6 Functional
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 212209 0 None -85 4 Mouse 6.6 pEC50 = 6.6 Functional
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 184972 0 None 1 4 Mouse 6.6 pEC50 = 6.6 Functional
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 184972 0 None 1 4 Mouse 6.6 pEC50 = 6.6 Functional
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 211026 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
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 125706 0 None -27 3 Human 5.6 pEC50 = 5.6 Functional
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 125706 0 None -27 3 Human 5.6 pEC50 = 5.6 Functional
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 208221 0 None -85 2 Human 5.6 pEC50 = 5.6 Functional
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 93698 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
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 93698 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
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 195138 0 None -23 4 Mouse 4.6 pEC50 = 4.6 Functional
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 195138 0 None -23 4 Mouse 4.6 pEC50 = 4.6 Functional
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 118296 0 None -64 4 Human 5.6 pEC50 = 5.6 Functional
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 118296 0 None -64 4 Human 5.6 pEC50 = 5.6 Functional
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 211888 0 None -39 4 Mouse 5.6 pEC50 = 5.6 Functional
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 191644 0 None -16 4 Human 6.6 pEC50 = 6.6 Functional
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 191644 0 None -16 4 Human 6.6 pEC50 = 6.6 Functional
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 138143 0 None -23 3 Human 5.6 pEC50 = 5.6 Functional
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 138143 0 None -23 3 Human 5.6 pEC50 = 5.6 Functional
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 212348 2 None -15 7 Human 6.6 pEC50 = 6.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 3747 37 None -239 7 Human 5.6 pEC50 = 5.6 Functional
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 94532 0 None -147 3 Human 6.6 pEC50 = 6.6 Functional
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 94532 0 None -147 3 Human 6.6 pEC50 = 6.6 Functional
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 188235 0 None -12 3 Human 7.6 pEC50 = 7.6 Functional
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 188235 0 None -12 3 Human 7.6 pEC50 = 7.6 Functional
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 2649 49 None -58 8 Human 7.6 pEC50 = 7.6 Functional
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 2649 49 None -58 8 Human 7.6 pEC50 = 7.6 Functional
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 2649 49 None -58 8 Human 7.6 pEC50 = 7.6 Functional
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 211095 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
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 210419 3 None -91 4 Mouse 6.6 pEC50 = 6.6 Functional
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 14891 0 None -91 4 Human 5.6 pEC50 = 5.6 Functional
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 14891 0 None -91 4 Human 5.6 pEC50 = 5.6 Functional
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 213847 0 None -17 4 Human 5.6 pEC50 = 5.6 Functional
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 156461 0 None -34 3 Mouse 5.6 pEC50 = 5.6 Functional
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 156461 0 None -34 3 Mouse 5.6 pEC50 = 5.6 Functional
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 156966 0 None -1 3 Mouse 5.6 pEC50 = 5.6 Functional
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 156966 0 None -1 3 Mouse 5.6 pEC50 = 5.6 Functional
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 166302 0 None -4 4 Human 6.6 pEC50 = 6.6 Functional
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 166302 0 None -4 4 Human 6.6 pEC50 = 6.6 Functional
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 207779 0 None -85 4 Mouse 5.6 pEC50 = 5.6 Functional
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 166133 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
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 166133 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
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 195699 0 None -48 2 Mouse 4.6 pEC50 = 4.6 Functional
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 195699 0 None -48 2 Mouse 4.6 pEC50 = 4.6 Functional
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 172759 0 None -8 3 Mouse 7.6 pEC50 = 7.6 Functional
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 172759 0 None -8 3 Mouse 7.6 pEC50 = 7.6 Functional
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 195759 0 None -2630 5 Mouse 7.6 pEC50 = 7.6 Functional
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 195759 0 None -2630 5 Mouse 7.6 pEC50 = 7.6 Functional
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 79867 0 None -18 3 Human 6.6 pEC50 = 6.6 Functional
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 79867 0 None -18 3 Human 6.6 pEC50 = 6.6 Functional
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 159163 0 None -14 4 Mouse 6.6 pEC50 = 6.6 Functional
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 159163 0 None -14 4 Mouse 6.6 pEC50 = 6.6 Functional
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 118652 0 None -537 5 Mouse 6.6 pEC50 = 6.6 Functional
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 118652 0 None -537 5 Mouse 6.6 pEC50 = 6.6 Functional
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 154300 0 None -69 3 Human 6.6 pEC50 = 6.6 Functional
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 154300 0 None -69 3 Human 6.6 pEC50 = 6.6 Functional
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 211904 0 None -19 3 Human 5.6 pEC50 = 5.6 Functional
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 77592 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
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 77592 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
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 67678 0 None -363 4 Mouse 6.6 pEC50 = 6.6 Functional
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 67678 0 None -363 4 Mouse 6.6 pEC50 = 6.6 Functional
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 158775 0 None -11 4 Human 5.6 pEC50 = 5.6 Functional
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 158775 0 None -11 4 Human 5.6 pEC50 = 5.6 Functional
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 158061 0 None -64 4 Human 4.6 pEC50 = 4.6 Functional
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 158061 0 None -64 4 Human 4.6 pEC50 = 4.6 Functional
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 211604 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
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 168365 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
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 168365 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
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 210521 0 None -97 5 Mouse 7.6 pEC50 = 7.6 Functional
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 207524 0 None -144 4 Human 7.6 pEC50 = 7.6 Functional
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 173233 0 None -4 4 Mouse 6.6 pEC50 = 6.6 Functional
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 173233 0 None -4 4 Mouse 6.6 pEC50 = 6.6 Functional
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 176151 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
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 176151 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
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 164146 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
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 164146 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
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 125156 0 None -331 4 Mouse 6.6 pEC50 = 6.6 Functional
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 125156 0 None -331 4 Mouse 6.6 pEC50 = 6.6 Functional
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 204878 0 None -14 3 Human 7.6 pEC50 = 7.6 Functional
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 204878 0 None -14 3 Human 7.6 pEC50 = 7.6 Functional
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 182289 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
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 182289 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
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 210565 0 None -18 3 Human 5.6 pEC50 = 5.6 Functional
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 186009 0 None -5 3 Mouse 5.6 pEC50 = 5.6 Functional
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 186009 0 None -5 3 Mouse 5.6 pEC50 = 5.6 Functional
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 195219 0 None -24 4 Mouse 4.6 pEC50 = 4.6 Functional
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 195219 0 None -24 4 Mouse 4.6 pEC50 = 4.6 Functional
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 158775 0 None -11 4 Human 6.6 pEC50 = 6.6 Functional
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 158775 0 None -11 4 Human 6.6 pEC50 = 6.6 Functional
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 77712 0 None -10 3 Human 6.5 pEC50 = 6.5 Functional
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 77712 0 None -10 3 Human 6.5 pEC50 = 6.5 Functional
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 153768 0 None 6 2 Human 7.5 pEC50 = 7.5 Functional
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 153768 0 None 6 2 Human 7.5 pEC50 = 7.5 Functional
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 182289 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
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 182289 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
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 96880 0 None -186 4 Mouse 7.5 pEC50 = 7.5 Functional
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 96880 0 None -186 4 Mouse 7.5 pEC50 = 7.5 Functional
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 96880 0 None -186 4 Mouse 7.5 pEC50 = 7.5 Functional
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 159197 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
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 159197 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
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 13878 0 None -57 3 Human 5.5 pEC50 = 5.5 Functional
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 13878 0 None -57 3 Human 5.5 pEC50 = 5.5 Functional
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 13878 0 None -57 3 Human 5.5 pEC50 = 5.5 Functional
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 191877 0 None -158 4 Human 6.5 pEC50 = 6.5 Functional
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 191877 0 None -158 4 Human 6.5 pEC50 = 6.5 Functional
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 154153 0 None -41 3 Human 5.5 pEC50 = 5.5 Functional
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 154153 0 None -41 3 Human 5.5 pEC50 = 5.5 Functional
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 137849 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
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 137849 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
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 96568 0 None -60 3 Human 8.5 pEC50 = 8.5 Functional
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 96568 0 None -60 3 Human 8.5 pEC50 = 8.5 Functional
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 211072 0 None -25 5 Rat 8.5 pEC50 = 8.5 Functional
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 2649 49 None -58 8 Human 8.5 pEC50 = 8.5 Functional
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 2649 49 None -58 8 Human 8.5 pEC50 = 8.5 Functional
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 2649 49 None -58 8 Human 8.5 pEC50 = 8.5 Functional
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 115736 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
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 115736 0 None -1 4 Mouse 8.5 pEC50 = 8.5 Functional
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 163753 0 None 18 4 Human 8.5 pEC50 = 8.5 Functional
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 163753 0 None 18 4 Human 8.5 pEC50 = 8.5 Functional
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 115729 0 None -4 4 Mouse 8.5 pEC50 = 8.5 Functional
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 115729 0 None -4 4 Mouse 8.5 pEC50 = 8.5 Functional
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 213704 0 None -42 4 Human 8.5 pEC50 = 8.5 Functional
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 115732 0 None -4 4 Mouse 8.4 pEC50 = 8.4 Functional
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 115732 0 None -4 4 Mouse 8.4 pEC50 = 8.4 Functional
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 115740 0 None -6 4 Mouse 8.4 pEC50 = 8.4 Functional
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 115740 0 None -6 4 Mouse 8.4 pEC50 = 8.4 Functional
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 1473 6 None 1 4 Human 8.4 pEC50 = 8.4 Functional
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 1473 6 None 1 4 Human 8.4 pEC50 = 8.4 Functional
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 1473 6 None 1 4 Human 8.4 pEC50 = 8.4 Functional
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 163154 0 None 6 3 Human 7.5 pEC50 = 7.5 Functional
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 163154 0 None 6 3 Human 7.5 pEC50 = 7.5 Functional
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 172509 0 None -151 4 Mouse 7.5 pEC50 = 7.5 Functional
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 172509 0 None -151 4 Mouse 7.5 pEC50 = 7.5 Functional
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 155940 0 None -10 3 Human 7.5 pEC50 = 7.5 Functional
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 155940 0 None -10 3 Human 7.5 pEC50 = 7.5 Functional
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 139394 0 None -7 5 Mouse 7.5 pEC50 = 7.5 Functional
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 139394 0 None -7 5 Mouse 7.5 pEC50 = 7.5 Functional
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 210524 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
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 189398 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
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 189398 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
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 158482 0 None -144 4 Mouse 6.5 pEC50 = 6.5 Functional
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 158482 0 None -144 4 Mouse 6.5 pEC50 = 6.5 Functional
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 211322 0 None -40 4 Human 6.5 pEC50 = 6.5 Functional
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 106628 0 None -42 3 Human 6.5 pEC50 = 6.5 Functional
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 106628 0 None -42 3 Human 6.5 pEC50 = 6.5 Functional
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 156286 0 None -66 4 Mouse 5.5 pEC50 = 5.5 Functional
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 156286 0 None -66 4 Mouse 5.5 pEC50 = 5.5 Functional
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 159089 0 None -56 3 Mouse 5.5 pEC50 = 5.5 Functional
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 159089 0 None -56 3 Mouse 5.5 pEC50 = 5.5 Functional
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 173124 0 None -125 4 Mouse 5.5 pEC50 = 5.5 Functional
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 173124 0 None -125 4 Mouse 5.5 pEC50 = 5.5 Functional
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 209553 0 None -52 5 Mouse 5.5 pEC50 = 5.5 Functional
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 174047 0 None -8 3 Mouse 4.5 pEC50 = 4.5 Functional
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 174047 0 None -8 3 Mouse 4.5 pEC50 = 4.5 Functional
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 195762 0 None -97 4 Mouse 4.5 pEC50 = 4.5 Functional
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 195762 0 None -97 4 Mouse 4.5 pEC50 = 4.5 Functional
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 66620 0 None -288 3 Human 5.5 pEC50 = 5.5 Functional
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 66620 0 None -288 3 Human 5.5 pEC50 = 5.5 Functional
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 7988 0 None -169 4 Human 5.5 pEC50 = 5.5 Functional
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 7988 0 None -169 4 Human 5.5 pEC50 = 5.5 Functional
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 7988 0 None -169 4 Human 5.5 pEC50 = 5.5 Functional
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 97452 0 None -17 3 Mouse 4.5 pEC50 = 4.5 Functional
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 97452 0 None -17 3 Mouse 4.5 pEC50 = 4.5 Functional
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 207309 0 None -89 3 Human 5.5 pEC50 = 5.5 Functional
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 207883 0 None -5 4 Mouse 6.5 pEC50 = 6.5 Functional
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 157771 0 None -416 4 Human 6.5 pEC50 = 6.5 Functional
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 157771 0 None -416 4 Human 6.5 pEC50 = 6.5 Functional
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 208863 1 None -35 8 Mouse 7.5 pEC50 = 7.5 Functional
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 211134 0 None -56 5 Rat 7.5 pEC50 = 7.5 Functional
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 185037 0 None 1 2 Mouse 6.5 pEC50 = 6.5 Functional
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 185037 0 None 1 2 Mouse 6.5 pEC50 = 6.5 Functional
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 138410 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
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 138410 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
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 122388 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
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 122388 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
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 166550 0 None -4 3 Human 6.5 pEC50 = 6.5 Functional
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 166550 0 None -4 3 Human 6.5 pEC50 = 6.5 Functional
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 77710 0 None -6 3 Human 5.5 pEC50 = 5.5 Functional
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 77710 0 None -6 3 Human 5.5 pEC50 = 5.5 Functional
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 156117 0 None -91 4 Mouse 7.5 pEC50 = 7.5 Functional
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 156117 0 None -91 4 Mouse 7.5 pEC50 = 7.5 Functional
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 97043 0 None -6 4 Mouse 6.5 pEC50 = 6.5 Functional
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 97043 0 None -6 4 Mouse 6.5 pEC50 = 6.5 Functional
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 58494 0 None -13 4 Mouse 5.5 pEC50 = 5.5 Functional
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 58494 0 None -13 4 Mouse 5.5 pEC50 = 5.5 Functional
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 58494 0 None -13 4 Mouse 5.5 pEC50 = 5.5 Functional
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 58494 0 None -13 4 Mouse 5.5 pEC50 = 5.5 Functional
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 58498 0 None -35 4 Mouse 6.5 pEC50 = 6.5 Functional
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 58498 0 None -35 4 Mouse 6.5 pEC50 = 6.5 Functional
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 58498 0 None -35 4 Mouse 6.5 pEC50 = 6.5 Functional
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 58498 0 None -35 4 Mouse 6.5 pEC50 = 6.5 Functional
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 58498 0 None -35 4 Mouse 6.5 pEC50 = 6.5 Functional
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 122040 0 None -30 4 Human 6.5 pEC50 = 6.5 Functional
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 122040 0 None -30 4 Human 6.5 pEC50 = 6.5 Functional
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 163282 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
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 163282 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
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 2649 49 None -58 8 Human 7.5 pEC50 = 7.5 Functional
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 2649 49 None -58 8 Human 7.5 pEC50 = 7.5 Functional
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 2649 49 None -58 8 Human 7.5 pEC50 = 7.5 Functional
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 188183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 195222 0 None -51 4 Mouse 4.5 pEC50 = 4.5 Functional
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 195222 0 None -51 4 Mouse 4.5 pEC50 = 4.5 Functional
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 125852 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 125852 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 210806 15 None -22 7 Mouse 7.5 pEC50 = 7.5 Functional
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 210806 15 None -22 7 Mouse 7.5 pEC50 = 7.5 Functional
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 138373 0 None -112 3 Human 6.5 pEC50 = 6.5 Functional
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 138373 0 None -112 3 Human 6.5 pEC50 = 6.5 Functional
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 206724 0 None -30 4 Mouse 4.5 pEC50 = 4.5 Functional
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 111250 0 None -41 5 Mouse 7.5 pEC50 = 7.5 Functional
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 111250 0 None -41 5 Mouse 7.5 pEC50 = 7.5 Functional
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 209659 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 173039 0 None -6 3 Mouse 6.5 pEC50 = 6.5 Functional
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 173039 0 None -6 3 Mouse 6.5 pEC50 = 6.5 Functional
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 184900 0 None 1 2 Mouse 6.5 pEC50 = 6.5 Functional
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 184900 0 None 1 2 Mouse 6.5 pEC50 = 6.5 Functional
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 214122 0 None -11 3 Human 6.5 pEC50 = 6.5 Functional
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 8308 3 None -85 7 Human 6.5 pEC50 = 6.5 Functional
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 8308 3 None -85 7 Human 6.5 pEC50 = 6.5 Functional
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 182244 0 None -21 3 Mouse 7.4 pEC50 = 7.4 Functional
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 182244 0 None -21 3 Mouse 7.4 pEC50 = 7.4 Functional
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 211057 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
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 185297 0 None -2 4 Mouse 6.4 pEC50 = 6.4 Functional
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 185297 0 None -2 4 Mouse 6.4 pEC50 = 6.4 Functional
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 185982 0 None 2 2 Mouse 6.4 pEC50 = 6.4 Functional
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 185982 0 None 2 2 Mouse 6.4 pEC50 = 6.4 Functional
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 7721 0 None -512 3 Human 5.4 pEC50 = 5.4 Functional
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 7721 0 None -512 3 Human 5.4 pEC50 = 5.4 Functional
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 7987 0 None -123 3 Human 5.4 pEC50 = 5.4 Functional
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 7987 0 None -123 3 Human 5.4 pEC50 = 5.4 Functional
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 212195 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
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 138696 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
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 138696 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
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 75036 0 None -218 4 Human 6.4 pEC50 = 6.4 Functional
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 75036 0 None -218 4 Human 6.4 pEC50 = 6.4 Functional
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 208414 0 None -1412 4 Human 6.4 pEC50 = 6.4 Functional
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 183845 0 None -1 3 Mouse 6.4 pEC50 = 6.4 Functional
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 183845 0 None -1 3 Mouse 6.4 pEC50 = 6.4 Functional
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 184561 0 None -12 3 Mouse 5.4 pEC50 = 5.4 Functional
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 184561 0 None -12 3 Mouse 5.4 pEC50 = 5.4 Functional
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 79148 0 None -467 3 Human 5.4 pEC50 = 5.4 Functional
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 79148 0 None -467 3 Human 5.4 pEC50 = 5.4 Functional
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 208863 1 None -35 8 Mouse 7.4 pEC50 = 7.4 Functional
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 213705 0 None -46 4 Human 7.4 pEC50 = 7.4 Functional
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 191074 0 None -234 4 Human 6.4 pEC50 = 6.4 Functional
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 191074 0 None -234 4 Human 6.4 pEC50 = 6.4 Functional
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 180062 0 None -43 3 Mouse 7.4 pEC50 = 7.4 Functional
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 180062 0 None -43 3 Mouse 7.4 pEC50 = 7.4 Functional
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 208853 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
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 191300 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
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 191300 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
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 213230 0 None -4 4 Human 7.4 pEC50 = 7.4 Functional
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 214128 0 None -35 3 Human 6.4 pEC50 = 6.4 Functional
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 158793 0 None -41 3 Mouse 5.4 pEC50 = 5.4 Functional
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 158793 0 None -41 3 Mouse 5.4 pEC50 = 5.4 Functional
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 58492 0 None -20 4 Mouse 5.4 pEC50 = 5.4 Functional
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 58492 0 None -20 4 Mouse 5.4 pEC50 = 5.4 Functional
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 58492 0 None -20 4 Mouse 5.4 pEC50 = 5.4 Functional
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 58492 0 None -20 4 Mouse 5.4 pEC50 = 5.4 Functional
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 122039 0 None -13 4 Human 5.4 pEC50 = 5.4 Functional
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 122039 0 None -13 4 Human 5.4 pEC50 = 5.4 Functional
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 212745 0 None -72 4 Human 6.4 pEC50 = 6.4 Functional
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 173611 0 None -13 4 Mouse 8.4 pEC50 = 8.4 Functional
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 173611 0 None -13 4 Mouse 8.4 pEC50 = 8.4 Functional
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 212917 0 None -4 4 Human 8.4 pEC50 = 8.4 Functional
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 163206 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
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 163206 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 299 23 None -16 9 Human 8.4 pEC50 = 8.4 Functional
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 212077 0 None -1 3 Human 8.4 pEC50 = 8.4 Functional
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 141006 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
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 141006 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
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 167409 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
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 167409 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
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 168890 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
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 168890 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
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 158705 0 None -131 4 Mouse 7.4 pEC50 = 7.4 Functional
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 158705 0 None -131 4 Mouse 7.4 pEC50 = 7.4 Functional
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 155630 0 None -275 4 Mouse 7.4 pEC50 = 7.4 Functional
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 155630 0 None -275 4 Mouse 7.4 pEC50 = 7.4 Functional
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 173342 0 None -13 4 Mouse 7.4 pEC50 = 7.4 Functional
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 173342 0 None -13 4 Mouse 7.4 pEC50 = 7.4 Functional
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 173844 0 None -56 4 Mouse 7.4 pEC50 = 7.4 Functional
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 173844 0 None -56 4 Mouse 7.4 pEC50 = 7.4 Functional
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 181648 0 None -36 3 Mouse 7.4 pEC50 = 7.4 Functional
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 181648 0 None -36 3 Mouse 7.4 pEC50 = 7.4 Functional
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 105484 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
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 105484 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
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 181983 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
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 181983 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
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 210998 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 157408 0 None -19 2 Mouse 5.4 pEC50 = 5.4 Functional
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 157408 0 None -19 2 Mouse 5.4 pEC50 = 5.4 Functional
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 171052 0 None -13 4 Mouse 5.4 pEC50 = 5.4 Functional
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 171052 0 None -13 4 Mouse 5.4 pEC50 = 5.4 Functional
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 185369 0 None -6 3 Mouse 5.4 pEC50 = 5.4 Functional
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 185369 0 None -6 3 Mouse 5.4 pEC50 = 5.4 Functional
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 156734 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 156734 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 207769 0 None -75 4 Mouse 5.4 pEC50 = 5.4 Functional
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 79386 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
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 79386 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
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 125774 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
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 125774 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
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 209486 0 None -79 4 Mouse 5.4 pEC50 = 5.4 Functional
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 7682 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
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 7682 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
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 7682 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
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 120973 0 None -74 4 Mouse 6.4 pEC50 = 6.4 Functional
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 120973 0 None -74 4 Mouse 6.4 pEC50 = 6.4 Functional
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 97588 0 None -18 3 Mouse 5.4 pEC50 = 5.4 Functional
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 97588 0 None -18 3 Mouse 5.4 pEC50 = 5.4 Functional
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 77661 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
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 77661 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
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 166922 0 None 5 3 Human 7.4 pEC50 = 7.4 Functional
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 166922 0 None 5 3 Human 7.4 pEC50 = 7.4 Functional
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 209659 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
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 185616 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
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 185616 0 None 1 3 Mouse 6.4 pEC50 = 6.4 Functional
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 96150 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
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 96150 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
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 210558 0 None 1 2 Human 5.4 pEC50 = 5.4 Functional
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 185912 0 None -14 3 Mouse 5.4 pEC50 = 5.4 Functional
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 185912 0 None -14 3 Mouse 5.4 pEC50 = 5.4 Functional
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 154152 0 None -18 3 Human 6.4 pEC50 = 6.4 Functional
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 154152 0 None -18 3 Human 6.4 pEC50 = 6.4 Functional
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 190472 0 None -22 4 Human 6.4 pEC50 = 6.4 Functional
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 190472 0 None -22 4 Human 6.4 pEC50 = 6.4 Functional
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 212348 2 None -138 7 Mouse 5.4 pEC50 = 5.4 Functional
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 212348 2 None -138 7 Mouse 5.4 pEC50 = 5.4 Functional
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 195760 0 None -8709 5 Mouse 4.4 pEC50 = 4.4 Functional
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 195760 0 None -8709 5 Mouse 4.4 pEC50 = 4.4 Functional
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 171978 0 None -48 3 Human 7.4 pEC50 = 7.4 Functional
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 171978 0 None -48 3 Human 7.4 pEC50 = 7.4 Functional
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 173205 0 None -36 3 Human 7.4 pEC50 = 7.4 Functional
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 173205 0 None -36 3 Human 7.4 pEC50 = 7.4 Functional
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 165604 0 None -13 4 Mouse 7.4 pEC50 = 7.4 Functional
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 165604 0 None -13 4 Mouse 7.4 pEC50 = 7.4 Functional
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 175080 0 None -144 3 Mouse 5.4 pEC50 = 5.4 Functional
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 175080 0 None -144 3 Mouse 5.4 pEC50 = 5.4 Functional
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 102288 0 None -1 4 Mouse 5.4 pEC50 = 5.4 Functional
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 102288 0 None -1 4 Mouse 5.4 pEC50 = 5.4 Functional
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 201648 0 None 1 3 Mouse 5.4 pEC50 = 5.4 Functional
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 201648 0 None 1 3 Mouse 5.4 pEC50 = 5.4 Functional
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 173736 0 None -630 3 Mouse 4.4 pEC50 = 4.4 Functional
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 173736 0 None -630 3 Mouse 4.4 pEC50 = 4.4 Functional
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 209454 0 None -10 4 Mouse 4.4 pEC50 = 4.4 Functional
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 207307 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
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 155534 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
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 155534 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
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 140830 0 None -316 4 Human 6.4 pEC50 = 6.4 Functional
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 140830 0 None -316 4 Human 6.4 pEC50 = 6.4 Functional
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 156841 0 None -58 3 Human 6.4 pEC50 = 6.4 Functional
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 156841 0 None -58 3 Human 6.4 pEC50 = 6.4 Functional
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 207770 0 None -2290 4 Mouse 5.4 pEC50 = 5.4 Functional
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 124128 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
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 124128 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
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 191048 0 None -213 4 Human 6.3 pEC50 = 6.3 Functional
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 191048 0 None -213 4 Human 6.3 pEC50 = 6.3 Functional
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 8194 0 None -102 2 Human 5.3 pEC50 = 5.3 Functional
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 8194 0 None -102 2 Human 5.3 pEC50 = 5.3 Functional
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 158034 0 None -18 4 Mouse 6.3 pEC50 = 6.3 Functional
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 158034 0 None -18 4 Mouse 6.3 pEC50 = 6.3 Functional
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 167810 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
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 167810 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
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 58498 0 None -35 4 Mouse 5.3 pEC50 = 5.3 Functional
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 58498 0 None -35 4 Mouse 5.3 pEC50 = 5.3 Functional
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 58498 0 None -35 4 Mouse 5.3 pEC50 = 5.3 Functional
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 58498 0 None -35 4 Mouse 5.3 pEC50 = 5.3 Functional
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 58498 0 None -35 4 Mouse 5.3 pEC50 = 5.3 Functional
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 210070 0 None -1 4 Human 6.3 pEC50 = 6.3 Functional
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 156522 0 None -131 4 Human 6.3 pEC50 = 6.3 Functional
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 156522 0 None -131 4 Human 6.3 pEC50 = 6.3 Functional
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 111252 0 None -42 5 Mouse 7.3 pEC50 = 7.3 Functional
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 111252 0 None -42 5 Mouse 7.3 pEC50 = 7.3 Functional
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 139108 0 None -380 5 Mouse 7.3 pEC50 = 7.3 Functional
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 139108 0 None -380 5 Mouse 7.3 pEC50 = 7.3 Functional
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 121635 0 None -12 3 Human 6.3 pEC50 = 6.3 Functional
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 121635 0 None -12 3 Human 6.3 pEC50 = 6.3 Functional
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 207776 0 None -97 4 Mouse 7.3 pEC50 = 7.3 Functional
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 8246 0 None -81 2 Human 6.3 pEC50 = 6.3 Functional
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 8246 0 None -81 2 Human 6.3 pEC50 = 6.3 Functional
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 58497 0 None -15 4 Mouse 6.3 pEC50 = 6.3 Functional
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 58497 0 None -15 4 Mouse 6.3 pEC50 = 6.3 Functional
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 58497 0 None -15 4 Mouse 6.3 pEC50 = 6.3 Functional
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 58497 0 None -15 4 Mouse 6.3 pEC50 = 6.3 Functional
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 121634 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
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 121634 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
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 163968 0 None 27 3 Human 8.3 pEC50 = 8.3 Functional
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 163968 0 None 27 3 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 155439 0 None -15 3 Human 8.3 pEC50 = 8.3 Functional
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 155439 0 None -15 3 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 2649 49 None -58 8 Human 8.3 pEC50 = 8.3 Functional
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 70775 0 None -12 4 Mouse 8.3 pEC50 = 8.3 Functional
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 70775 0 None -12 4 Mouse 8.3 pEC50 = 8.3 Functional
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 210833 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
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 208526 0 None -53 4 Human 8.3 pEC50 = 8.3 Functional
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 79961 0 None -3 3 Human 8.3 pEC50 = 8.3 Functional
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 79961 0 None -3 3 Human 8.3 pEC50 = 8.3 Functional
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 1473 6 None 1 4 Human 8.2 pEC50 = 8.2 Functional
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 1473 6 None 1 4 Human 8.2 pEC50 = 8.2 Functional
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 1473 6 None 1 4 Human 8.2 pEC50 = 8.2 Functional
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 188420 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
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 188420 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
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 173749 0 None -20 3 Mouse 7.3 pEC50 = 7.3 Functional
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 173749 0 None -20 3 Mouse 7.3 pEC50 = 7.3 Functional
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 175199 0 None -3 4 Mouse 7.3 pEC50 = 7.3 Functional
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 175199 0 None -3 4 Mouse 7.3 pEC50 = 7.3 Functional
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 175523 0 None -83 4 Mouse 7.3 pEC50 = 7.3 Functional
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 175523 0 None -83 4 Mouse 7.3 pEC50 = 7.3 Functional
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 8195 0 None -15 3 Human 6.3 pEC50 = 6.3 Functional
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 8195 0 None -15 3 Human 6.3 pEC50 = 6.3 Functional
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 175220 0 None -38 4 Mouse 6.3 pEC50 = 6.3 Functional
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 175220 0 None -38 4 Mouse 6.3 pEC50 = 6.3 Functional
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 155781 0 None -1 2 Mouse 5.3 pEC50 = 5.3 Functional
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 155781 0 None -1 2 Mouse 5.3 pEC50 = 5.3 Functional
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 174377 0 None -28 3 Mouse 4.3 pEC50 = 4.3 Functional
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 174377 0 None -28 3 Mouse 4.3 pEC50 = 4.3 Functional
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 190081 0 None -125 4 Human 6.3 pEC50 = 6.3 Functional
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 190081 0 None -125 4 Human 6.3 pEC50 = 6.3 Functional
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 188117 0 None -30 3 Human 7.3 pEC50 = 7.3 Functional
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 188117 0 None -30 3 Human 7.3 pEC50 = 7.3 Functional
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 174487 0 None -51 3 Mouse 7.3 pEC50 = 7.3 Functional
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 174487 0 None -51 3 Mouse 7.3 pEC50 = 7.3 Functional
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 156997 0 None -30 4 Mouse 6.3 pEC50 = 6.3 Functional
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 156997 0 None -30 4 Mouse 6.3 pEC50 = 6.3 Functional
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 122041 0 None -10 4 Human 5.3 pEC50 = 5.3 Functional
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 122041 0 None -10 4 Human 5.3 pEC50 = 5.3 Functional
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 118294 0 None -4 4 Human 7.3 pEC50 = 7.3 Functional
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 118294 0 None -4 4 Human 7.3 pEC50 = 7.3 Functional
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 172779 0 None -19 3 Human 7.3 pEC50 = 7.3 Functional
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 172779 0 None -19 3 Human 7.3 pEC50 = 7.3 Functional
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 1473 6 None 1 4 Human 6.3 pEC50 = 6.3 Functional
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 1473 6 None 1 4 Human 6.3 pEC50 = 6.3 Functional
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 1473 6 None 1 4 Human 6.3 pEC50 = 6.3 Functional
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 185192 0 None -7 3 Mouse 5.3 pEC50 = 5.3 Functional
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 185192 0 None -7 3 Mouse 5.3 pEC50 = 5.3 Functional
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 212395 0 None -99 4 Mouse 6.3 pEC50 = 6.3 Functional
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 212182 0 None -120 4 Mouse 7.3 pEC50 = 7.3 Functional
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 155675 0 None -13 4 Human 5.3 pEC50 = 5.3 Functional
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 155675 0 None -13 4 Human 5.3 pEC50 = 5.3 Functional
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 75051 0 None -186 4 Human 6.3 pEC50 = 6.3 Functional
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 75051 0 None -186 4 Human 6.3 pEC50 = 6.3 Functional
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 159024 0 None -33 4 Mouse 6.3 pEC50 = 6.3 Functional
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 159024 0 None -33 4 Mouse 6.3 pEC50 = 6.3 Functional
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 79334 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
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 79334 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
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 79334 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
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 79334 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
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 188336 0 None -69 3 Human 6.3 pEC50 = 6.3 Functional
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 188336 0 None -69 3 Human 6.3 pEC50 = 6.3 Functional
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 118298 0 None -1 4 Human 7.3 pEC50 = 7.3 Functional
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 118298 0 None -1 4 Human 7.3 pEC50 = 7.3 Functional
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 111254 0 None -87 5 Mouse 7.3 pEC50 = 7.3 Functional
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 111254 0 None -87 5 Mouse 7.3 pEC50 = 7.3 Functional
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 208863 1 None -35 8 Mouse 7.3 pEC50 = 7.3 Functional
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 139814 0 None -54 4 Human 6.3 pEC50 = 6.3 Functional
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 139814 0 None -54 4 Human 6.3 pEC50 = 6.3 Functional
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 207740 0 None -3 4 Mouse 5.3 pEC50 = 5.3 Functional
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 207299 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
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 64226 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
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 64226 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
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 188237 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
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 188237 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
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 212808 0 None -25 4 Human 7.3 pEC50 = 7.3 Functional
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 138144 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
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 138144 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
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 166491 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
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 166491 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
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 156351 0 None 1 4 Mouse 7.2 pEC50 = 7.2 Functional
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 156351 0 None 1 4 Mouse 7.2 pEC50 = 7.2 Functional
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 8192 0 None -95 3 Human 6.2 pEC50 = 6.2 Functional
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 8192 0 None -95 3 Human 6.2 pEC50 = 6.2 Functional
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 106514 0 None -60 3 Human 6.2 pEC50 = 6.2 Functional
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 106514 0 None -60 3 Human 6.2 pEC50 = 6.2 Functional
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 172127 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
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 172127 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
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 111081 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
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 111081 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
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 195605 0 None -54 4 Mouse 4.2 pEC50 = 4.2 Functional
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 195605 0 None -54 4 Mouse 4.2 pEC50 = 4.2 Functional
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 31077 0 None -138 3 Human 7.2 pEC50 = 7.2 Functional
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 31077 0 None -138 3 Human 7.2 pEC50 = 7.2 Functional
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 208479 0 None -1 3 Rat 7.2 pEC50 = 7.2 Functional
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 140023 0 None -134 4 Human 6.2 pEC50 = 6.2 Functional
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 140023 0 None -134 4 Human 6.2 pEC50 = 6.2 Functional
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 137021 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
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 137021 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
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 141017 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
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 141017 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
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 174762 0 None -30 4 Mouse 8.2 pEC50 = 8.2 Functional
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 174762 0 None -30 4 Mouse 8.2 pEC50 = 8.2 Functional
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 93620 0 None -15 4 Human 8.2 pEC50 = 8.2 Functional
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 93620 0 None -15 4 Human 8.2 pEC50 = 8.2 Functional
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 162818 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
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 162818 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
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 208222 0 None -47 4 Human 8.2 pEC50 = 8.2 Functional
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 208222 0 None -47 4 Human 8.2 pEC50 = 8.2 Functional
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 212934 0 None -9 4 Human 8.2 pEC50 = 8.2 Functional
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 213479 0 None -8 4 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 207534 31 None -7 8 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 299 23 None -16 9 Human 8.2 pEC50 = 8.2 Functional
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 210809 0 None -39 4 Mouse 8.2 pEC50 = 8.2 Functional
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 172317 0 None -30 4 Mouse 7.2 pEC50 = 7.2 Functional
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 172317 0 None -30 4 Mouse 7.2 pEC50 = 7.2 Functional
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 172522 0 None -30 3 Mouse 7.2 pEC50 = 7.2 Functional
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 172522 0 None -30 3 Mouse 7.2 pEC50 = 7.2 Functional
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 174723 0 None -12 4 Mouse 7.2 pEC50 = 7.2 Functional
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 174723 0 None -12 4 Mouse 7.2 pEC50 = 7.2 Functional
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 182256 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
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 182256 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
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 7727 0 None -151 2 Human 6.2 pEC50 = 6.2 Functional
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 7727 0 None -151 2 Human 6.2 pEC50 = 6.2 Functional
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 156864 0 None -70 4 Mouse 6.2 pEC50 = 6.2 Functional
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 156864 0 None -70 4 Mouse 6.2 pEC50 = 6.2 Functional
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 174795 0 None -15 4 Mouse 5.2 pEC50 = 5.2 Functional
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 174795 0 None -15 4 Mouse 5.2 pEC50 = 5.2 Functional
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 182256 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
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 182256 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
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 156925 0 None -158 4 Mouse 6.2 pEC50 = 6.2 Functional
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 156925 0 None -158 4 Mouse 6.2 pEC50 = 6.2 Functional
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 212218 0 None -47 4 Mouse 6.2 pEC50 = 6.2 Functional
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 213770 0 None -16 3 Human 6.2 pEC50 = 6.2 Functional
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 185385 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
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 185385 0 None -6 3 Mouse 5.2 pEC50 = 5.2 Functional
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 155697 0 None -69 3 Human 6.2 pEC50 = 6.2 Functional
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 155697 0 None -69 3 Human 6.2 pEC50 = 6.2 Functional
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 208754 0 None -977 4 Mouse 4.2 pEC50 = 4.2 Functional
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 211136 0 None -457 5 Rat 7.2 pEC50 = 7.2 Functional
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 75068 0 None -120 4 Human 6.2 pEC50 = 6.2 Functional
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 75068 0 None -120 4 Human 6.2 pEC50 = 6.2 Functional
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 204804 0 None -46 3 Human 6.2 pEC50 = 6.2 Functional
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 204804 0 None -46 3 Human 6.2 pEC50 = 6.2 Functional
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 122799 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
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 122799 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
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 189976 0 None -61 4 Human 6.2 pEC50 = 6.2 Functional
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 189976 0 None -61 4 Human 6.2 pEC50 = 6.2 Functional
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 7673 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
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 7673 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
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 182321 0 None -4 3 Mouse 7.2 pEC50 = 7.2 Functional
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 182321 0 None -4 3 Mouse 7.2 pEC50 = 7.2 Functional
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 211431 0 None -77 5 Rat 6.2 pEC50 = 6.2 Functional
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 207306 0 None -16 3 Human 5.2 pEC50 = 5.2 Functional
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 122800 0 None -25 3 Human 6.2 pEC50 = 6.2 Functional
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 122800 0 None -25 3 Human 6.2 pEC50 = 6.2 Functional
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 139549 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
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 139549 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
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 153871 0 None -77 3 Human 6.2 pEC50 = 6.2 Functional
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 153871 0 None -77 3 Human 6.2 pEC50 = 6.2 Functional
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 156555 0 None -1202 4 Human 5.2 pEC50 = 5.2 Functional
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 156555 0 None -1202 4 Human 5.2 pEC50 = 5.2 Functional
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 208863 1 None -3 8 Human 8.2 pEC50 = 8.2 Functional
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 210877 0 None -66 5 Rat 8.1 pEC50 = 8.1 Functional
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 212708 0 None -57 4 Human 8.1 pEC50 = 8.1 Functional
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 181599 0 None -1 3 Mouse 7.2 pEC50 = 7.2 Functional
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 181599 0 None -1 3 Mouse 7.2 pEC50 = 7.2 Functional
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 173231 0 None -7 3 Mouse 6.2 pEC50 = 6.2 Functional
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 173231 0 None -7 3 Mouse 6.2 pEC50 = 6.2 Functional
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 1473 6 None 1 4 Human 6.2 pEC50 = 6.2 Functional
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 1473 6 None 1 4 Human 6.2 pEC50 = 6.2 Functional
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 1473 6 None 1 4 Human 6.2 pEC50 = 6.2 Functional
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 63998 0 None -2511 3 Human 5.2 pEC50 = 5.2 Functional
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 63998 0 None -2511 3 Human 5.2 pEC50 = 5.2 Functional
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 121914 0 None -7 4 Human 6.2 pEC50 = 6.2 Functional
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 121914 0 None -7 4 Human 6.2 pEC50 = 6.2 Functional
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 7672 0 None -4 3 Human 7.2 pEC50 = 7.2 Functional
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 7672 0 None -4 3 Human 7.2 pEC50 = 7.2 Functional
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 111889 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
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 111889 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
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 207781 0 None -446 4 Mouse 5.2 pEC50 = 5.2 Functional
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 199398 0 None -891 4 Mouse 5.1 pEC50 = 5.1 Functional
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 199398 0 None -891 4 Mouse 5.1 pEC50 = 5.1 Functional
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 212608 0 None -512 4 Human 7.1 pEC50 = 7.1 Functional
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 173284 0 None -18 4 Mouse 6.1 pEC50 = 6.1 Functional
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 173284 0 None -18 4 Mouse 6.1 pEC50 = 6.1 Functional
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 157312 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
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 157312 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
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 163795 0 None -1 4 Human 7.1 pEC50 = 7.1 Functional
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 163795 0 None -1 4 Human 7.1 pEC50 = 7.1 Functional
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 208863 1 None -35 8 Mouse 7.1 pEC50 = 7.1 Functional
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 195575 0 None -6 4 Mouse 5.1 pEC50 = 5.1 Functional
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 195575 0 None -6 4 Mouse 5.1 pEC50 = 5.1 Functional
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 157002 0 None -5 4 Human 5.1 pEC50 = 5.1 Functional
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 157002 0 None -5 4 Human 5.1 pEC50 = 5.1 Functional
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 7722 0 None -354 3 Human 5.1 pEC50 = 5.1 Functional
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 7722 0 None -354 3 Human 5.1 pEC50 = 5.1 Functional
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 7722 0 None -354 3 Human 5.1 pEC50 = 5.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 299 23 None -7 9 Mouse 7.1 pEC50 = 7.1 Functional
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 210879 0 None -34 5 Rat 7.1 pEC50 = 7.1 Functional
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 209659 0 None 1 3 Human 6.1 pEC50 = 6.1 Functional
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 210078 0 None -4 4 Human 6.1 pEC50 = 6.1 Functional
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 131966 0 None -53 3 Human 6.1 pEC50 = 6.1 Functional
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 131966 0 None -53 3 Human 6.1 pEC50 = 6.1 Functional
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 157419 0 None -1445 4 Human 6.1 pEC50 = 6.1 Functional
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 157419 0 None -1445 4 Human 6.1 pEC50 = 6.1 Functional
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 163397 0 None -6 4 Human 7.1 pEC50 = 7.1 Functional
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 163397 0 None -6 4 Human 7.1 pEC50 = 7.1 Functional
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 163489 0 None -1 4 Human 7.1 pEC50 = 7.1 Functional
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 163489 0 None -1 4 Human 7.1 pEC50 = 7.1 Functional
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 58495 0 None -46 4 Mouse 5.1 pEC50 = 5.1 Functional
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 58495 0 None -46 4 Mouse 5.1 pEC50 = 5.1 Functional
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 14969 0 None -257 5 Human 6.1 pEC50 = 6.1 Functional
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 14969 0 None -257 5 Human 6.1 pEC50 = 6.1 Functional
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 181085 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
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 181085 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
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 181085 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
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 181085 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
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 122043 0 None -3 4 Human 6.1 pEC50 = 6.1 Functional
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 122043 0 None -3 4 Human 6.1 pEC50 = 6.1 Functional
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 157340 0 None -194 5 Mouse 6.1 pEC50 = 6.1 Functional
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 157340 0 None -194 5 Mouse 6.1 pEC50 = 6.1 Functional
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 212256 0 None -15 4 Mouse 6.1 pEC50 = 6.1 Functional
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 207773 0 None 1 4 Mouse 5.1 pEC50 = 5.1 Functional
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 97293 0 None -1548 5 Mouse 5.1 pEC50 = 5.1 Functional
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 97293 0 None -1548 5 Mouse 5.1 pEC50 = 5.1 Functional
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 4524 0 None -12 4 Mouse 5.1 pEC50 = 5.1 Functional
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 4524 0 None -12 4 Mouse 5.1 pEC50 = 5.1 Functional
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 14872 0 None -13 4 Human 7.1 pEC50 = 7.1 Functional
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 14872 0 None -13 4 Human 7.1 pEC50 = 7.1 Functional
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 172610 0 None -13 4 Mouse 8.1 pEC50 = 8.1 Functional
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 172610 0 None -13 4 Mouse 8.1 pEC50 = 8.1 Functional
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 174513 0 None -15 4 Mouse 6.1 pEC50 = 6.1 Functional
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 174513 0 None -15 4 Mouse 6.1 pEC50 = 6.1 Functional
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 210077 0 None -1 4 Human 6.1 pEC50 = 6.1 Functional
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 207778 0 None -426 4 Mouse 5.1 pEC50 = 5.1 Functional
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 157216 0 None -38 2 Human 6.1 pEC50 = 6.1 Functional
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 157216 0 None -38 2 Human 6.1 pEC50 = 6.1 Functional
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 137098 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
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 137098 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
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 123563 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
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 123563 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
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 79774 0 None -38 3 Human 7.1 pEC50 = 7.1 Functional
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 79774 0 None -38 3 Human 7.1 pEC50 = 7.1 Functional
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 171428 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
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 171428 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
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 212306 0 None -213 5 Mouse 7.1 pEC50 = 7.1 Functional
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 153554 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
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 153554 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
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 214119 0 None -38 3 Human 6.1 pEC50 = 6.1 Functional
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 172374 0 None -18 3 Human 6.1 pEC50 = 6.1 Functional
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 172374 0 None -18 3 Human 6.1 pEC50 = 6.1 Functional
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 138119 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
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 138119 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
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 120972 0 None -22 4 Mouse 6.1 pEC50 = 6.1 Functional
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 120972 0 None -22 4 Mouse 6.1 pEC50 = 6.1 Functional
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 165435 0 None -4 3 Human 6.1 pEC50 = 6.1 Functional
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 165435 0 None -4 3 Human 6.1 pEC50 = 6.1 Functional
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 207237 0 None -10 3 Human 7.1 pEC50 = 7.1 Functional
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 66433 0 None -63 3 Human 6.1 pEC50 = 6.1 Functional
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 66433 0 None -63 3 Human 6.1 pEC50 = 6.1 Functional
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 155559 0 None -295 4 Human 5.1 pEC50 = 5.1 Functional
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 155559 0 None -295 4 Human 5.1 pEC50 = 5.1 Functional
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 139274 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
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 139274 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
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 211061 0 None -38 3 Human 7.1 pEC50 = 7.1 Functional
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 140138 0 None -77 4 Human 6.1 pEC50 = 6.1 Functional
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 140138 0 None -77 4 Human 6.1 pEC50 = 6.1 Functional
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 14873 0 None -83 4 Human 6.1 pEC50 = 6.1 Functional
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 14873 0 None -83 4 Human 6.1 pEC50 = 6.1 Functional
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 96122 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
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 96122 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
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 155690 0 None 2 2 Mouse 5.1 pEC50 = 5.1 Functional
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 155690 0 None 2 2 Mouse 5.1 pEC50 = 5.1 Functional
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 67677 0 None -28 4 Mouse 8.0 pEC50 = 8.0 Functional
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 67677 0 None -28 4 Mouse 8.0 pEC50 = 8.0 Functional
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 205452 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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 205452 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
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 190885 0 None 1 4 Human 8.0 pEC50 = 8.0 Functional
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 190885 0 None 1 4 Human 8.0 pEC50 = 8.0 Functional
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 210071 0 None 1 4 Human 8.0 pEC50 = 8 Functional
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 14870 0 None -16 4 Human 7.1 pEC50 = 7.1 Functional
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 14870 0 None -16 4 Human 7.1 pEC50 = 7.1 Functional
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 191531 2 None -52 4 Human 6.0 pEC50 = 6.0 Functional
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 191531 2 None -52 4 Human 6.0 pEC50 = 6.0 Functional
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 207311 0 None -30 3 Human 6.0 pEC50 = 6.0 Functional
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 94627 0 None -218 3 Human 6.0 pEC50 = 6.0 Functional
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 94627 0 None -218 3 Human 6.0 pEC50 = 6.0 Functional
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 210060 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
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 209951 0 None -57 4 Mouse 5.0 pEC50 = 5.0 Functional
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 96284 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
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 96284 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
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 158087 0 None -6 4 Mouse 6.0 pEC50 = 6.0 Functional
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 158087 0 None -6 4 Mouse 6.0 pEC50 = 6.0 Functional
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 111255 0 None -93 5 Mouse 7.0 pEC50 = 7.0 Functional
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 111255 0 None -93 5 Mouse 7.0 pEC50 = 7.0 Functional
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 94384 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
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 94384 0 None 8 2 Human 7.0 pEC50 = 7.0 Functional
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 213526 0 None -26 4 Human 7.0 pEC50 = 7.0 Functional
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 211408 0 None -154 4 Human 6.0 pEC50 = 6.0 Functional
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 212348 2 None -138 7 Mouse 6.0 pEC50 = 6.0 Functional
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 126258 0 None -13 3 Human 6.0 pEC50 = 6.0 Functional
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 126258 0 None -13 3 Human 6.0 pEC50 = 6.0 Functional
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 166903 0 None -109 3 Human 7.0 pEC50 = 7.0 Functional
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 166903 0 None -109 3 Human 7.0 pEC50 = 7.0 Functional
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 207482 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
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 106668 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
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 106668 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
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 171931 0 None -38 3 Human 6.0 pEC50 = 6.0 Functional
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 171931 0 None -38 3 Human 6.0 pEC50 = 6.0 Functional
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 75156 0 None -134 4 Human 6.0 pEC50 = 6 Functional
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 75156 0 None -134 4 Human 6.0 pEC50 = 6 Functional
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 130849 2 None -144 4 Human 6.0 pEC50 = 6 Functional
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 130849 2 None -144 4 Human 6.0 pEC50 = 6 Functional
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 4524 0 None -12 4 Mouse 5.0 pEC50 = 5 Functional
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 4524 0 None -12 4 Mouse 5.0 pEC50 = 5 Functional
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 65882 0 None -33 3 Human 6.0 pEC50 = 6 Functional
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 65882 0 None -33 3 Human 6.0 pEC50 = 6 Functional
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 8308 3 None -151 7 Rat 6.0 pEC50 = 6 Functional
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 8308 3 None -151 7 Rat 6.0 pEC50 = 6 Functional
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 208226 0 None -63 4 Human 8.0 pIC50 = 8.0 Functional
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 208226 0 None -63 4 Human 8.0 pIC50 = 8.0 Functional
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 208222 0 None -47 4 Human 8.0 pIC50 = 8.0 Functional
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 208222 0 None -47 4 Human 8.0 pIC50 = 8.0 Functional
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 182400 0 None -20 2 Human 6.0 pIC50 = 6 Functional
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 182400 0 None -20 2 Human 6.0 pIC50 = 6 Functional
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 182400 0 None -20 2 Human 6.0 pIC50 = 6 Functional
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 182400 0 None -20 2 Human 6.0 pIC50 = 6 Functional
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 182946 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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 182946 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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 182946 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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 182946 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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 181611 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
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 181611 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
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 181223 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
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 181223 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
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 181223 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
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 181223 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
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 189798 1 None -4 2 Human 5.7 pIC50 = 5.7 Functional
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 189798 1 None -4 2 Human 5.7 pIC50 = 5.7 Functional
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 189798 1 None -4 2 Human 5.7 pIC50 = 5.7 Functional
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 189798 1 None -4 2 Human 5.7 pIC50 = 5.7 Functional
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 182008 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 182008 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 182008 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 182008 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 182732 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
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 182732 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
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 182732 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
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 182732 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
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 181767 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
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 181767 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
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 181767 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
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 181767 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
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 182542 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
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 182542 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
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 182542 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
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 182542 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
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 181955 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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 181955 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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 181955 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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 181955 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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 182679 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
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 182679 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
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 182679 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
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 182679 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
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 181324 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 181324 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 181324 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 181324 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 182476 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 182476 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 182476 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 182476 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
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 182380 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
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 182380 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
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 182380 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
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 182380 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
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 181129 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 181129 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 181129 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 181129 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 182878 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
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 182878 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
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 182878 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
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 182878 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
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 182439 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
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 182439 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
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 182439 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
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 182439 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
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 182871 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182871 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182975 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
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 182975 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
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 182975 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
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 182975 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
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 182871 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182871 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 181142 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
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 181142 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
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 181142 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
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 181142 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
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 182471 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182471 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182471 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 182471 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 3543 12 None -125 5 Human 7.1 pIC50 = 7.1 Functional
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 181611 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
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 181611 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
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 208764 0 None - 0 Human 10.6 pKd = 10.6 Functional
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 207777 0 None - 3 Mouse 9.9 pKd = 9.9 Functional
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 153771 0 None 2 3 Human 9.8 pKd = 9.8 Functional
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 153771 0 None 2 3 Human 9.8 pKd = 9.8 Functional
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 121913 0 None 1 4 Human 9.1 pKd = 9.1 Functional
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 121913 0 None 1 4 Human 9.1 pKd = 9.1 Functional
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 185144 0 None - 0 Mouse 9.0 pKd = 9 Functional
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 185144 0 None - 0 Mouse 9.0 pKd = 9 Functional
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 96515 0 None - 1 Mouse 8.9 pKd = 8.9 Functional
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 184137 0 None - 0 Mouse 8.8 pKd = 8.8 Functional
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 184137 0 None - 0 Mouse 8.8 pKd = 8.8 Functional
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 135913 0 None - 1 Mouse 8.8 pKd = 8.8 Functional
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 135913 0 None - 1 Mouse 8.8 pKd = 8.8 Functional
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 207462 0 None -3 6 Human 8.7 pKd = 8.7 Functional
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 184262 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
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 184262 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
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 121919 0 None -2 4 Human 8.0 pKd = 8 Functional
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 121919 0 None -2 4 Human 8.0 pKd = 8 Functional
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 162426 0 None - 0 Mouse 8.0 pKd = 8 Functional
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 162426 0 None - 0 Mouse 8.0 pKd = 8 Functional
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 185165 0 None - 0 Mouse 8.0 pKd = 8 Functional
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 185165 0 None - 0 Mouse 8.0 pKd = 8 Functional
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 184137 0 None - 0 Mouse 7.0 pKd = 7 Functional
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 184137 0 None - 0 Mouse 7.0 pKd = 7 Functional
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 186018 0 None - 0 Mouse 7.0 pKd = 7 Functional
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 186018 0 None - 0 Mouse 7.0 pKd = 7 Functional
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 178870 0 None - 1 Mouse 6.0 pKd = 6 Functional
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 178870 0 None - 1 Mouse 6.0 pKd = 6 Functional
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 185604 0 None - 1 Mouse 6.0 pKd = 6 Functional
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 185604 0 None - 1 Mouse 6.0 pKd = 6 Functional
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 185899 0 None - 0 Mouse 6.0 pKd = 6 Functional
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 185899 0 None - 0 Mouse 6.0 pKd = 6 Functional
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 161714 0 None - 1 Mouse 7.9 pKd = 7.9 Functional
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 161714 0 None - 1 Mouse 7.9 pKd = 7.9 Functional
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 179475 0 None - 0 Mouse 6.9 pKd = 6.9 Functional
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 179475 0 None - 0 Mouse 6.9 pKd = 6.9 Functional
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 180889 0 None - 2 Mouse 6.9 pKd = 6.9 Functional
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 180889 0 None - 2 Mouse 6.9 pKd = 6.9 Functional
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 184016 0 None - 1 Mouse 6.9 pKd = 6.9 Functional
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 184016 0 None - 1 Mouse 6.9 pKd = 6.9 Functional
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 184867 0 None - 1 Mouse 6.9 pKd = 6.9 Functional
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 184867 0 None - 1 Mouse 6.9 pKd = 6.9 Functional
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 182784 0 None - 0 Mouse 5.9 pKd = 5.9 Functional
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 182784 0 None - 0 Mouse 5.9 pKd = 5.9 Functional
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 158890 0 None - 0 Mouse 5.9 pKd = 5.9 Functional
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 158890 0 None - 0 Mouse 5.9 pKd = 5.9 Functional
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 173237 0 None -1380 5 Mouse 5.9 pKd = 5.9 Functional
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 173237 0 None -1380 5 Mouse 5.9 pKd = 5.9 Functional
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 185144 0 None - 0 Mouse 7.8 pKd = 7.8 Functional
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 185144 0 None - 0 Mouse 7.8 pKd = 7.8 Functional
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 185008 0 None - 1 Mouse 7.8 pKd = 7.8 Functional
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 185008 0 None - 1 Mouse 7.8 pKd = 7.8 Functional
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 162283 0 None - 1 Mouse 6.8 pKd = 6.8 Functional
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 162283 0 None - 1 Mouse 6.8 pKd = 6.8 Functional
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 185004 0 None - 0 Mouse 6.8 pKd = 6.8 Functional
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 185004 0 None - 0 Mouse 6.8 pKd = 6.8 Functional
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 185165 0 None - 0 Mouse 6.8 pKd = 6.8 Functional
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 185165 0 None - 0 Mouse 6.8 pKd = 6.8 Functional
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 208636 0 None -14 3 Mouse 6.8 pKd = 6.8 Functional
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 181832 0 None - 1 Mouse 5.8 pKd = 5.8 Functional
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 181832 0 None - 1 Mouse 5.8 pKd = 5.8 Functional
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 156041 0 None - 2 Mouse 5.8 pKd = 5.8 Functional
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 156041 0 None - 2 Mouse 5.8 pKd = 5.8 Functional
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 171139 0 None - 2 Mouse 5.8 pKd = 5.8 Functional
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 171139 0 None - 2 Mouse 5.8 pKd = 5.8 Functional
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 183875 0 None - 0 Mouse 5.8 pKd = 5.8 Functional
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 183875 0 None - 0 Mouse 5.8 pKd = 5.8 Functional
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 185532 0 None - 1 Mouse 5.8 pKd = 5.8 Functional
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 185532 0 None - 1 Mouse 5.8 pKd = 5.8 Functional
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 212372 0 None - 3 Mouse 6.8 pKd = 6.8 Functional
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 162207 0 None - 0 Mouse 7.7 pKd = 7.7 Functional
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 162207 0 None - 0 Mouse 7.7 pKd = 7.7 Functional
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 185451 0 None - 0 Mouse 7.7 pKd = 7.7 Functional
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 185451 0 None - 0 Mouse 7.7 pKd = 7.7 Functional
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 158372 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 158372 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 208863 1 None -35 8 Mouse 6.7 pKd = 6.7 Functional
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 212244 0 None - 2 Mouse 6.7 pKd = 6.7 Functional
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 161643 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 161643 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 161736 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 161736 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 156316 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 156316 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 183875 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 183875 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 184671 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 184671 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 185317 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 185317 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 185915 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 185915 0 None - 0 Mouse 6.7 pKd = 6.7 Functional
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 157826 0 None - 1 Mouse 5.7 pKd = 5.7 Functional
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 157826 0 None - 1 Mouse 5.7 pKd = 5.7 Functional
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 155895 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 155895 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 155983 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 155983 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 184810 0 None - 1 Mouse 5.7 pKd = 5.7 Functional
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 184810 0 None - 1 Mouse 5.7 pKd = 5.7 Functional
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 184892 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 184892 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 186018 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 186018 0 None - 0 Mouse 5.7 pKd = 5.7 Functional
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 208167 0 None - 2 Mouse 5.7 pKd = 5.7 Functional
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 184194 0 None - 1 Mouse 8.6 pKd = 8.6 Functional
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 184194 0 None - 1 Mouse 8.6 pKd = 8.6 Functional
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 184278 0 None - 1 Mouse 8.6 pKd = 8.6 Functional
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 184278 0 None - 1 Mouse 8.6 pKd = 8.6 Functional
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 207775 0 None - 3 Mouse 7.6 pKd = 7.6 Functional
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 185189 0 None - 0 Mouse 7.6 pKd = 7.6 Functional
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 185189 0 None - 0 Mouse 7.6 pKd = 7.6 Functional
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 185899 0 None - 0 Mouse 7.6 pKd = 7.6 Functional
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 185899 0 None - 0 Mouse 7.6 pKd = 7.6 Functional
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 161458 0 None - 1 Mouse 6.6 pKd = 6.6 Functional
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 161458 0 None - 1 Mouse 6.6 pKd = 6.6 Functional
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 184767 0 None - 1 Mouse 6.6 pKd = 6.6 Functional
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 184767 0 None - 1 Mouse 6.6 pKd = 6.6 Functional
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 184892 0 None - 0 Mouse 6.6 pKd = 6.6 Functional
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 184892 0 None - 0 Mouse 6.6 pKd = 6.6 Functional
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 155162 0 None - 4 Mouse 5.6 pKd = 5.6 Functional
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 155162 0 None - 4 Mouse 5.6 pKd = 5.6 Functional
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 179100 0 None - 0 Mouse 5.6 pKd = 5.6 Functional
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 179100 0 None - 0 Mouse 5.6 pKd = 5.6 Functional
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 156054 0 None - 1 Mouse 5.6 pKd = 5.6 Functional
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 156054 0 None - 1 Mouse 5.6 pKd = 5.6 Functional
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 156996 0 None - 2 Mouse 5.6 pKd = 5.6 Functional
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 156996 0 None - 2 Mouse 5.6 pKd = 5.6 Functional
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 157352 0 None - 1 Mouse 5.6 pKd = 5.6 Functional
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 157352 0 None - 1 Mouse 5.6 pKd = 5.6 Functional
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 184081 0 None - 0 Mouse 5.6 pKd = 5.6 Functional
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 184081 0 None - 0 Mouse 5.6 pKd = 5.6 Functional
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 212378 0 None - 3 Mouse 7.5 pKd = 7.5 Functional
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 206717 0 None -100 4 Mouse 6.5 pKd = 6.5 Functional
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 121917 0 None -1 4 Human 8.5 pKd = 8.5 Functional
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 121917 0 None -1 4 Human 8.5 pKd = 8.5 Functional
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 184012 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 184012 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 184016 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 184016 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 184020 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 184020 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 135913 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 135913 0 None - 1 Mouse 8.5 pKd = 8.5 Functional
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 211327 0 None 1 4 Human 8.4 pKd = 8.4 Functional
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 158966 0 None -1659 5 Mouse 6.5 pKd = 6.5 Functional
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 158966 0 None -1659 5 Mouse 6.5 pKd = 6.5 Functional
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 161935 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
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 161935 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
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 162107 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
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 162107 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
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 184020 0 None - 1 Mouse 7.5 pKd = 7.5 Functional
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 184020 0 None - 1 Mouse 7.5 pKd = 7.5 Functional
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 158966 0 None -1659 5 Mouse 6.5 pKd = 6.5 Functional
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 158966 0 None -1659 5 Mouse 6.5 pKd = 6.5 Functional
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 161789 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 161789 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 162534 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 162534 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 174401 0 None -208 5 Mouse 6.5 pKd = 6.5 Functional
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 174401 0 None -208 5 Mouse 6.5 pKd = 6.5 Functional
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 156054 0 None - 1 Mouse 6.5 pKd = 6.5 Functional
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 156054 0 None - 1 Mouse 6.5 pKd = 6.5 Functional
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 179913 0 None - 0 Mouse 5.5 pKd = 5.5 Functional
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 179913 0 None - 0 Mouse 5.5 pKd = 5.5 Functional
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 185451 0 None - 0 Mouse 5.5 pKd = 5.5 Functional
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 185451 0 None - 0 Mouse 5.5 pKd = 5.5 Functional
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 159178 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 159178 0 None - 0 Mouse 6.5 pKd = 6.5 Functional
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 212366 0 None - 3 Mouse 7.4 pKd = 7.4 Functional
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 209488 0 None - 4 Mouse 7.4 pKd = 7.4 Functional
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 184012 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
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 184012 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
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 184262 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
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 184262 0 None - 1 Mouse 7.4 pKd = 7.4 Functional
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 156403 0 None - 0 Mouse 6.4 pKd = 6.4 Functional
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 156403 0 None - 0 Mouse 6.4 pKd = 6.4 Functional
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 158703 0 None - 1 Mouse 5.4 pKd = 5.4 Functional
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 158703 0 None - 1 Mouse 5.4 pKd = 5.4 Functional
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 172958 0 None -15 5 Mouse 5.4 pKd = 5.4 Functional
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 172958 0 None -15 5 Mouse 5.4 pKd = 5.4 Functional
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 96627 0 None 1 4 Human 8.3 pKd = 8.3 Functional
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 96627 0 None 1 4 Human 8.3 pKd = 8.3 Functional
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 184727 0 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 184727 0 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 184867 0 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 184867 0 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 185004 0 None - 0 Mouse 8.3 pKd = 8.3 Functional
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 185004 0 None - 0 Mouse 8.3 pKd = 8.3 Functional
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 208938 0 None -83 6 Human 8.3 pKd = 8.3 Functional
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 211724 0 None -26 5 Human 8.3 pKd = 8.3 Functional
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 210002 1 None -245 5 Mouse 6.3 pKd = 6.3 Functional
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 161865 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
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 161865 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
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 210002 1 None -245 5 Mouse 6.3 pKd = 6.3 Functional
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 184767 0 None - 1 Mouse 6.3 pKd = 6.3 Functional
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 184767 0 None - 1 Mouse 6.3 pKd = 6.3 Functional
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 184810 0 None - 1 Mouse 6.3 pKd = 6.3 Functional
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 184810 0 None - 1 Mouse 6.3 pKd = 6.3 Functional
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 185564 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
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 185564 0 None - 0 Mouse 6.3 pKd = 6.3 Functional
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 159219 0 None - 1 Mouse 5.3 pKd = 5.3 Functional
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 159219 0 None - 1 Mouse 5.3 pKd = 5.3 Functional
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 209488 0 None - 4 Mouse 7.3 pKd = 7.3 Functional
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 210074 0 None -2 4 Human 8.2 pKd = 8.2 Functional
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 185604 0 None - 1 Mouse 8.2 pKd = 8.2 Functional
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 185604 0 None - 1 Mouse 8.2 pKd = 8.2 Functional
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 162406 0 None - 0 Mouse 7.2 pKd = 7.2 Functional
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 162406 0 None - 0 Mouse 7.2 pKd = 7.2 Functional
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 184278 0 None - 1 Mouse 7.2 pKd = 7.2 Functional
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 184278 0 None - 1 Mouse 7.2 pKd = 7.2 Functional
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 162389 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 162389 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 156596 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 156596 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 185008 0 None - 1 Mouse 6.2 pKd = 6.2 Functional
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 185008 0 None - 1 Mouse 6.2 pKd = 6.2 Functional
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 185189 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 185189 0 None - 0 Mouse 6.2 pKd = 6.2 Functional
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 139366 0 None -123 3 Mouse 6.1 pKd = 6.1 Functional
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 139366 0 None -123 3 Mouse 6.1 pKd = 6.1 Functional
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 179491 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 179491 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 161439 0 None - 0 Mouse 7.1 pKd = 7.1 Functional
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 161439 0 None - 0 Mouse 7.1 pKd = 7.1 Functional
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 161890 0 None - 0 Mouse 7.1 pKd = 7.1 Functional
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 161890 0 None - 0 Mouse 7.1 pKd = 7.1 Functional
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 162121 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 162121 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 162325 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 162325 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 184194 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 184194 0 None - 1 Mouse 7.1 pKd = 7.1 Functional
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 155761 0 None - 0 Mouse 6.1 pKd = 6.1 Functional
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 155761 0 None - 0 Mouse 6.1 pKd = 6.1 Functional
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 156054 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
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 156054 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
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 174367 0 None -1230 5 Mouse 6.1 pKd = 6.1 Functional
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 174367 0 None -1230 5 Mouse 6.1 pKd = 6.1 Functional
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 184671 0 None - 0 Mouse 6.1 pKd = 6.1 Functional
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 184671 0 None - 0 Mouse 6.1 pKd = 6.1 Functional
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 184727 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
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 184727 0 None - 1 Mouse 6.1 pKd = 6.1 Functional
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 166094 0 None - 1 Mouse 8.1 pKd = 8.1 Functional
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 166094 0 None - 1 Mouse 8.1 pKd = 8.1 Functional
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 166094 0 None - 1 Mouse 8.1 pKd = 8.1 Functional
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 139268 0 None -33 4 Mouse 6.1 pKd = 6.1 Functional
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 139268 0 None -33 4 Mouse 6.1 pKd = 6.1 Functional
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 139290 0 None -45 3 Mouse 6.1 pKd = 6.1 Functional
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 139290 0 None -45 3 Mouse 6.1 pKd = 6.1 Functional
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 206717 0 None -100 4 Mouse 6.0 pKd = 6.0 Functional
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 185144 0 None - 0 Mouse 9.0 pKi = 9 Functional
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 185144 0 None - 0 Mouse 9.0 pKi = 9 Functional
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 184137 0 None - 0 Mouse 8.8 pKi = 8.8 Functional
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 184137 0 None - 0 Mouse 8.8 pKi = 8.8 Functional
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 135913 0 None - 1 Mouse 8.8 pKi = 8.8 Functional
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 135913 0 None - 1 Mouse 8.8 pKi = 8.8 Functional
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 185165 0 None - 0 Mouse 8.0 pKi = 8 Functional
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 185165 0 None - 0 Mouse 8.0 pKi = 8 Functional
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 184137 0 None - 0 Mouse 7.0 pKi = 7 Functional
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 184137 0 None - 0 Mouse 7.0 pKi = 7 Functional
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 186018 0 None - 0 Mouse 7.0 pKi = 7 Functional
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 186018 0 None - 0 Mouse 7.0 pKi = 7 Functional
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 185604 0 None - 1 Mouse 6.0 pKi = 6 Functional
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 185604 0 None - 1 Mouse 6.0 pKi = 6 Functional
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 185899 0 None - 0 Mouse 6.0 pKi = 6 Functional
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 185899 0 None - 0 Mouse 6.0 pKi = 6 Functional
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 184016 0 None - 1 Mouse 6.9 pKi = 6.9 Functional
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 184016 0 None - 1 Mouse 6.9 pKi = 6.9 Functional
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 184867 0 None - 1 Mouse 6.9 pKi = 6.9 Functional
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 184867 0 None - 1 Mouse 6.9 pKi = 6.9 Functional
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 185144 0 None - 0 Mouse 7.8 pKi = 7.8 Functional
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 185144 0 None - 0 Mouse 7.8 pKi = 7.8 Functional
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 185008 0 None - 1 Mouse 7.8 pKi = 7.8 Functional
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 185008 0 None - 1 Mouse 7.8 pKi = 7.8 Functional
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 185004 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
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 185004 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
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 185165 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
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 185165 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
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 183875 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
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 183875 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
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 185532 0 None - 1 Mouse 5.8 pKi = 5.8 Functional
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 185532 0 None - 1 Mouse 5.8 pKi = 5.8 Functional
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 184262 0 None - 1 Mouse 8.7 pKi = 8.7 Functional
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 184262 0 None - 1 Mouse 8.7 pKi = 8.7 Functional
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 184194 0 None - 1 Mouse 8.6 pKi = 8.6 Functional
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 184194 0 None - 1 Mouse 8.6 pKi = 8.6 Functional
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 184278 0 None - 1 Mouse 8.6 pKi = 8.6 Functional
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 184278 0 None - 1 Mouse 8.6 pKi = 8.6 Functional
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 185451 0 None - 0 Mouse 7.7 pKi = 7.7 Functional
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 185451 0 None - 0 Mouse 7.7 pKi = 7.7 Functional
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 183875 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 183875 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 184671 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 184671 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 185317 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 185317 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 185915 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 185915 0 None - 0 Mouse 6.7 pKi = 6.7 Functional
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 184810 0 None - 1 Mouse 5.7 pKi = 5.7 Functional
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 184810 0 None - 1 Mouse 5.7 pKi = 5.7 Functional
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 184892 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
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 184892 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
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 186018 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
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 186018 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
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 185189 0 None - 0 Mouse 7.6 pKi = 7.6 Functional
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 185189 0 None - 0 Mouse 7.6 pKi = 7.6 Functional
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 185899 0 None - 0 Mouse 7.6 pKi = 7.6 Functional
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 185899 0 None - 0 Mouse 7.6 pKi = 7.6 Functional
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 184767 0 None - 1 Mouse 6.6 pKi = 6.6 Functional
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 184767 0 None - 1 Mouse 6.6 pKi = 6.6 Functional
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 184892 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
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 184892 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
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 155162 0 None - 4 Mouse 5.6 pKi = 5.6 Functional
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 155162 0 None - 4 Mouse 5.6 pKi = 5.6 Functional
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 184081 0 None - 0 Mouse 5.6 pKi = 5.6 Functional
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 184081 0 None - 0 Mouse 5.6 pKi = 5.6 Functional
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 209488 0 None - 4 Mouse 6.6 pKi = 6.6 Functional
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 212366 0 None - 3 Mouse 6.6 pKi = 6.6 Functional
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 184012 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184012 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184016 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184016 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184020 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184020 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 135913 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 135913 0 None - 1 Mouse 8.5 pKi = 8.5 Functional
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 184020 0 None - 1 Mouse 7.5 pKi = 7.5 Functional
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 184020 0 None - 1 Mouse 7.5 pKi = 7.5 Functional
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 156054 0 None - 1 Mouse 6.5 pKi = 6.5 Functional
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 156054 0 None - 1 Mouse 6.5 pKi = 6.5 Functional
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 185451 0 None - 0 Mouse 5.5 pKi = 5.5 Functional
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 185451 0 None - 0 Mouse 5.5 pKi = 5.5 Functional
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 212378 0 None - 3 Mouse 6.5 pKi = 6.5 Functional
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 184012 0 None - 1 Mouse 7.4 pKi = 7.4 Functional
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 184012 0 None - 1 Mouse 7.4 pKi = 7.4 Functional
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 184262 0 None - 1 Mouse 7.4 pKi = 7.4 Functional
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 184262 0 None - 1 Mouse 7.4 pKi = 7.4 Functional
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 184727 0 None - 1 Mouse 8.3 pKi = 8.3 Functional
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 184727 0 None - 1 Mouse 8.3 pKi = 8.3 Functional
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 184867 0 None - 1 Mouse 8.3 pKi = 8.3 Functional
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 184867 0 None - 1 Mouse 8.3 pKi = 8.3 Functional
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 185004 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
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 185004 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
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 184767 0 None - 1 Mouse 6.3 pKi = 6.3 Functional
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 184767 0 None - 1 Mouse 6.3 pKi = 6.3 Functional
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 184810 0 None - 1 Mouse 6.3 pKi = 6.3 Functional
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 184810 0 None - 1 Mouse 6.3 pKi = 6.3 Functional
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 185564 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
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 185564 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
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 212244 0 None - 2 Mouse 5.3 pKi = 5.3 Functional
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 185604 0 None - 1 Mouse 8.2 pKi = 8.2 Functional
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 185604 0 None - 1 Mouse 8.2 pKi = 8.2 Functional
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 212372 0 None - 3 Mouse 5.2 pKi = 5.2 Functional
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 184278 0 None - 1 Mouse 7.2 pKi = 7.2 Functional
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 184278 0 None - 1 Mouse 7.2 pKi = 7.2 Functional
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 185008 0 None - 1 Mouse 6.2 pKi = 6.2 Functional
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 185008 0 None - 1 Mouse 6.2 pKi = 6.2 Functional
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 185189 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
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 185189 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
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 184194 0 None - 1 Mouse 7.1 pKi = 7.1 Functional
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 184194 0 None - 1 Mouse 7.1 pKi = 7.1 Functional
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 156054 0 None - 1 Mouse 6.1 pKi = 6.1 Functional
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 156054 0 None - 1 Mouse 6.1 pKi = 6.1 Functional
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 184671 0 None - 0 Mouse 6.1 pKi = 6.1 Functional
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 184671 0 None - 0 Mouse 6.1 pKi = 6.1 Functional
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 184727 0 None - 1 Mouse 6.1 pKi = 6.1 Functional
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 184727 0 None - 1 Mouse 6.1 pKi = 6.1 Functional
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 210889 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
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 210889 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
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 210889 20 None -1 7 Mouse 8.0 pEC50 = 8.0 Functional
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 712 26 None -5 4 Human 8.1 pEC50 = 8.1 Functional
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 712 26 None -5 4 Human 8.1 pEC50 = 8.1 Functional
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 712 26 None -5 4 Human 8.1 pEC50 = 8.1 Functional
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 712 26 None -5 4 Human 8.1 pEC50 = 8.1 Functional
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 712 26 None -5 4 Human 8.1 pEC50 = 8.1 Functional
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 3026 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17482720
1334 1473 6 None 1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
16133814 1473 6 None 1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
CHEMBL437050 1473 6 None 1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
1341 3027 0 None -6 3 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1329 311 0 None - 1 Mouse 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
1335 312 0 None -39 3 Human 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9819197




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
1324 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
16154396 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
44285019 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
57514683 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
91898441 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL441738 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
DB04931 299 23 None - 4 Mouse 10.1 pEC50 = 10.1 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 299 23 None - 4 Mouse 10.0 pEC50 = 10.0 Binding
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 2649 49 None - 3 Mouse 9.9 pEC50 = 9.9 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
92432 2649 49 None - 3 Mouse 9.9 pEC50 = 9.9 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL430239 2649 49 None - 3 Mouse 9.9 pEC50 = 9.9 Binding
Effective concentration for mouse Melanocortin-3 receptorEffective concentration for mouse Melanocortin-3 receptor
ChEMBL None None None None 10.1021/jm049010r
1324 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 299 23 None -2 4 Human 9.9 pEC50 = 9.9 Binding
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 2649 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
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 2649 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
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 2649 49 None - 3 Mouse 9.8 pEC50 = 9.8 Binding
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 141331 0 None - 0 Mouse 9.8 pEC50 = 9.8 Binding
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 141331 0 None - 0 Mouse 9.8 pEC50 = 9.8 Binding
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 2649 49 None -72 3 Human 9.6 pEC50 = 9.6 Binding
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 2649 49 None -72 3 Human 9.6 pEC50 = 9.6 Binding
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 2649 49 None -72 3 Human 9.6 pEC50 = 9.6 Binding
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 2649 49 None - 3 Mouse 9.5 pEC50 = 9.5 Binding
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 2649 49 None - 3 Mouse 9.5 pEC50 = 9.5 Binding
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 2649 49 None - 3 Mouse 9.5 pEC50 = 9.5 Binding
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 207534 31 None - 4 Mouse 9.2 pEC50 = 9.2 Binding
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 207534 31 None - 4 Mouse 9.2 pEC50 = 9.2 Binding
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 207534 31 None - 4 Mouse 9.2 pEC50 = 9.2 Binding
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 207534 31 None - 4 Mouse 9.2 pEC50 = 9.2 Binding
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 207534 31 None -30 4 Human 9.2 pEC50 = 9.2 Binding
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 207534 31 None -30 4 Human 9.2 pEC50 = 9.2 Binding
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 207534 31 None -30 4 Human 9.2 pEC50 = 9.2 Binding
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 207534 31 None -30 4 Human 9.2 pEC50 = 9.2 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207534 31 None - 4 Mouse 9.1 pEC50 = 9.1 Binding
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 207995 0 None - 0 Mouse 9.0 pEC50 = 9.0 Binding
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 208056 0 None -1 3 Human 8.7 pEC50 = 8.7 Binding
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 106535 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 106535 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 211885 0 None - 0 Mouse 5.0 pEC50 = 5.0 Binding
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 214144 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
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 209548 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
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 106234 0 None -4 2 Human 7.9 pEC50 = 7.9 Binding
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 106234 0 None -4 2 Human 7.9 pEC50 = 7.9 Binding
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 208008 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
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 209966 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
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 208006 0 None - 0 Mouse 4.9 pEC50 = 4.9 Binding
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 208019 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
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 214131 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 207059 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 209480 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 44991 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
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 44991 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
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 208863 1 None -39 2 Mouse 6.8 pEC50 = 6.8 Binding
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 207315 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 207322 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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 210056 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 209965 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
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 209969 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 171314 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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 171314 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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 208012 0 None - 0 Mouse 4.8 pEC50 = 4.8 Binding
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 168430 0 None 7 3 Human 7.8 pEC50 = 7.8 Binding
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 168430 0 None 7 3 Human 7.8 pEC50 = 7.8 Binding
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 211874 0 None - 0 Mouse 4.7 pEC50 = 4.7 Binding
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 207313 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 210425 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 209964 0 None - 0 Mouse 4.7 pEC50 = 4.7 Binding
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 97886 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 97886 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 209461 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
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 207460 0 None - 0 Mouse 4.6 pEC50 = 4.6 Binding
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 208005 0 None - 0 Mouse 4.6 pEC50 = 4.6 Binding
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 210428 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 30046 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 30046 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 207055 0 None - 0 Mouse 4.6 pEC50 = 4.6 Binding
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 208003 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
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 209587 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
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 3543 12 None -12 7 Mouse 8.5 pEC50 = 8.5 Binding
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 3543 12 None -12 7 Mouse 8.5 pEC50 = 8.5 Binding
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 3543 12 None -12 7 Mouse 8.5 pEC50 = 8.5 Binding
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 3543 12 None -12 7 Mouse 8.5 pEC50 = 8.5 Binding
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 209973 0 None - 0 Mouse 4.5 pEC50 = 4.5 Binding
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 208013 0 None - 0 Mouse 4.5 pEC50 = 4.5 Binding
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 207310 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 207336 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 210290 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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 208018 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
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 208011 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
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 208272 0 None - 0 Mouse 4.5 pEC50 = 4.5 Binding
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 208002 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
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 207058 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
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 207052 0 None - 0 Mouse 5.4 pEC50 = 5.4 Binding
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 98042 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 98042 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 207998 0 None - 0 Mouse 4.4 pEC50 = 4.4 Binding
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 210294 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 210420 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 168154 0 None 1 2 Human 4.4 pEC50 = 4.4 Binding
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 168154 0 None 1 2 Human 4.4 pEC50 = 4.4 Binding
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 208001 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
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 155309 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
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 155309 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
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 207999 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
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 207318 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
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 207333 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 208389 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 207053 0 None - 0 Mouse 4.3 pEC50 = 4.3 Binding
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 208863 1 None -39 2 Mouse 5.3 pEC50 = 5.3 Binding
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 207739 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
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 209724 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
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 208000 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
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 214132 0 None - 0 Mouse 5.2 pEC50 = 5.2 Binding
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 207335 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 207317 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 207323 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 208863 1 None -39 2 Mouse 7.2 pEC50 = 7.2 Binding
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 167640 0 None 4 3 Human 7.2 pEC50 = 7.2 Binding
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 167640 0 None 4 3 Human 7.2 pEC50 = 7.2 Binding
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 210296 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 167493 0 None 7 3 Human 7.2 pEC50 = 7.2 Binding
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 167493 0 None 7 3 Human 7.2 pEC50 = 7.2 Binding
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 205199 0 None -13 3 Human 7.2 pEC50 = 7.2 Binding
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 205199 0 None -13 3 Human 7.2 pEC50 = 7.2 Binding
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 98077 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 98077 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 209996 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
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 105680 0 None 6 3 Human 7.1 pEC50 = 7.1 Binding
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 105680 0 None 6 3 Human 7.1 pEC50 = 7.1 Binding
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 200133 0 None -2 3 Human 6.1 pEC50 = 6.1 Binding
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 200133 0 None -2 3 Human 6.1 pEC50 = 6.1 Binding
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 207320 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 209585 0 None - 0 Mouse 5.1 pEC50 = 5.1 Binding
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 208272 0 None - 0 Mouse 5.0 pEC50 = 5 Binding
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 206766 0 None -1 2 Human 9.7 pIC50 = 9.7 Binding
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 10165 0 None -2 2 Human 9.7 pIC50 = 9.7 Binding
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 10165 0 None -2 2 Human 9.7 pIC50 = 9.7 Binding
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 207462 0 None -5 2 Human 9.6 pIC50 = 9.6 Binding
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 212353 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 299 23 None -2 4 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 163968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 163968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 168028 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 168028 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 210715 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
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 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
92432 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2649 49 None -72 3 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL204310 207420 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 121913 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
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 121913 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
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 211327 0 None -1 2 Human 8.8 pIC50 = 8.8 Binding
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 211724 0 None -100 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 163154 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 163154 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 118296 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 118296 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 211095 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 118298 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 118298 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 102658 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 102658 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 174367 0 None -31 4 Mouse 5.0 pIC50 = 5 Binding
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 174367 0 None -31 4 Mouse 5.0 pIC50 = 5 Binding
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 211061 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 139463 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
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 139463 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
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 166903 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 166903 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 121919 0 None 1 4 Human 7.0 pIC50 = 7.0 Binding
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 121919 0 None 1 4 Human 7.0 pIC50 = 7.0 Binding
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 163282 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 163282 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 153771 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
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 153771 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
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 166922 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 166922 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 206762 0 None -63 2 Human 7.0 pIC50 = 7.0 Binding
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 130849 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 130849 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 168365 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 168365 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 207461 0 None - 1 Mouse 4.9 pIC50 = 4.9 Binding
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 96627 0 None -2 2 Human 7.9 pIC50 = 7.9 Binding
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 96627 0 None -2 2 Human 7.9 pIC50 = 7.9 Binding
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 211590 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 167689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 167689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 210558 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 154832 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 154832 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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
176 394 63 None -6 31 Human 4.9 pIC50 = 4.9 Binding
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 394 63 None -6 31 Human 4.9 pIC50 = 4.9 Binding
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 394 63 None -6 31 Human 4.9 pIC50 = 4.9 Binding
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 394 63 None -6 31 Human 4.9 pIC50 = 4.9 Binding
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 394 63 None -6 31 Human 4.9 pIC50 = 4.9 Binding
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 210428 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 207313 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 207320 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 210011 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
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 122039 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 122039 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 207417 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 121922 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 121922 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 78071 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 78071 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 139366 0 None -177 3 Mouse 5.9 pIC50 = 5.9 Binding
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 139366 0 None -177 3 Mouse 5.9 pIC50 = 5.9 Binding
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 139108 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 139108 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 126260 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 126260 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 209733 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 163795 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 163795 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 208636 0 None -5 2 Mouse 6.9 pIC50 = 6.9 Binding
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 208845 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 210565 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 208414 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 206717 0 None -52 3 Mouse 5.8 pIC50 = 5.8 Binding
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 121918 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 121918 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 94532 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 94532 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 94827 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 94827 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 210074 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
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 120781 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 120781 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 151708 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 151708 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 172958 0 None -10 3 Mouse 4.8 pIC50 = 4.8 Binding
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 172958 0 None -10 3 Mouse 4.8 pIC50 = 4.8 Binding
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 502 77 None -147 41 Human 4.8 pIC50 = 4.8 Binding
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
249 502 77 None -147 41 Human 4.8 pIC50 = 4.8 Binding
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 502 77 None -147 41 Human 4.8 pIC50 = 4.8 Binding
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 502 77 None -147 41 Human 4.8 pIC50 = 4.8 Binding
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 502 77 None -147 41 Human 4.8 pIC50 = 4.8 Binding
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 207310 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 164105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 164105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 130849 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 130849 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 78566 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 78566 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 122041 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 122041 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 121912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 121912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 122450 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 122450 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 210002 1 None -31 3 Mouse 4.8 pIC50 = 4.8 Binding
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 32474 12 None -45 10 Human 4.8 pIC50 = 4.8 Binding
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 32474 12 None -45 10 Human 4.8 pIC50 = 4.8 Binding
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 32474 12 None -45 10 Human 4.8 pIC50 = 4.8 Binding
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 152515 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 152515 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 148521 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 148521 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 205195 91 None -54 34 Human 4.7 pIC50 = 4.7 Binding
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 205195 91 None -54 34 Human 4.7 pIC50 = 4.7 Binding
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 205195 91 None -54 34 Human 4.7 pIC50 = 4.7 Binding
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 3747 37 None - 4 Rat 5.7 pIC50 = 5.7 Binding
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 3747 37 None - 4 Rat 5.7 pIC50 = 5.7 Binding
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 3747 37 None - 4 Rat 5.7 pIC50 = 5.7 Binding
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 207534 31 None -30 4 Human 7.7 pIC50 = 7.7 Binding
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 207534 31 None -30 4 Human 7.7 pIC50 = 7.7 Binding
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 207534 31 None -30 4 Human 7.7 pIC50 = 7.7 Binding
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 207534 31 None -30 4 Human 7.7 pIC50 = 7.7 Binding
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 210070 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 206765 0 None -19 2 Human 6.7 pIC50 = 6.7 Binding
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 171888 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 171888 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 207482 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 207698 0 None 1 3 Human 6.7 pIC50 = 6.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 3690 75 None -56 35 Human 4.7 pIC50 = 4.7 Binding
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 210296 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 207321 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 207322 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 2649 49 None -72 3 Human 8.7 pIC50 = 8.7 Binding
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 212392 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 212172 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 163691 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 163691 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 212381 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 207462 0 None -5 2 Human 8.6 pIC50 = 8.6 Binding
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 212370 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 210469 1 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 206764 0 None 12 2 Human 8.6 pIC50 = 8.6 Binding
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 206767 0 None -5 2 Human 8.6 pIC50 = 8.6 Binding
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 121921 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 121921 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 207419 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 213847 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 163397 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 163397 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 122040 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 122040 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 153724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 153724 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 210066 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 78337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 78337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 67093 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 67093 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 75036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 75036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 66934 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 66934 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 66934 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 190577 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 190577 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 210076 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 166491 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 166491 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 143653 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 143653 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 207628 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 121878 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 121878 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 94414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 94414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 60485 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 60485 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 140137 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 140137 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 130849 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 130849 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 189976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 189976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 121915 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 121915 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 207632 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 906 64 None -186 72 Human 4.6 pIC50 = 4.6 Binding
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
621 906 64 None -186 72 Human 4.6 pIC50 = 4.6 Binding
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
83 906 64 None -186 72 Human 4.6 pIC50 = 4.6 Binding
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 906 64 None -186 72 Human 4.6 pIC50 = 4.6 Binding
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 906 64 None -186 72 Human 4.6 pIC50 = 4.6 Binding
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 190885 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 190885 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 161375 0 None -17 3 Human 7.6 pIC50 = 7.6 Binding
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 161375 0 None -17 3 Human 7.6 pIC50 = 7.6 Binding
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 161375 0 None -17 3 Human 7.6 pIC50 = 7.6 Binding
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 207464 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 207524 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 210524 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 156925 0 None - 1 Mouse 5.6 pIC50 = 5.6 Binding
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 156925 0 None - 1 Mouse 5.6 pIC50 = 5.6 Binding
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 163411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 163411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 210068 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 208418 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 207416 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 210545 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 209659 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 103715 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 103715 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 174401 0 None -10 4 Mouse 4.6 pIC50 = 4.6 Binding
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 174401 0 None -10 4 Mouse 4.6 pIC50 = 4.6 Binding
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 145391 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 145391 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 208527 0 None -316 2 Human 6.5 pIC50 = 6.5 Binding
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 157280 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 157280 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 116489 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 116489 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 94627 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 94627 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 95155 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 95155 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 208364 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 96195 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 96195 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 210069 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 207462 0 None -5 2 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
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 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16154396 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
44285019 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
57514683 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
91898441 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
DB04931 299 23 None -2 4 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL266417 208938 0 None -8 3 Human 8.5 pIC50 = 8.5 Binding
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 210065 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 299 23 None -2 4 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
145964017 163489 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 163489 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 207534 31 None -30 4 Human 7.5 pIC50 = 7.5 Binding
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 210973 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 191714 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 191714 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 96717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 96717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 75051 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 75051 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 207315 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 122449 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 122449 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 191531 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 191531 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 94413 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 94413 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 207753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 158966 0 None -138 3 Mouse 5.5 pIC50 = 5.5 Binding
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 158966 0 None -138 3 Mouse 5.5 pIC50 = 5.5 Binding
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 211847 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
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 60493 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 60493 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 210079 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 15435 4 None -309 8 Human 5.5 pIC50 = 5.5 Binding
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 15435 4 None -309 8 Human 5.5 pIC50 = 5.5 Binding
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 209659 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 158034 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 158034 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 139219 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
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 139219 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
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 139219 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
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 139268 0 None -52 3 Mouse 6.5 pIC50 = 6.5 Binding
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 139268 0 None -52 3 Mouse 6.5 pIC50 = 6.5 Binding
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 82842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 82842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 14862 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 14862 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 203802 73 None -75 34 Human 4.4 pIC50 = 4.4 Binding
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 203802 73 None -75 34 Human 4.4 pIC50 = 4.4 Binding
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 203802 73 None -75 34 Human 4.4 pIC50 = 4.4 Binding
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 210072 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 154709 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 154709 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 193798 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 193798 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 140023 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 140023 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 153768 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 153768 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 60492 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 60492 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 208419 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 207323 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 208392 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 210294 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 299 23 None - 4 Mouse 8.4 pIC50 = 8.4 Binding
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 164180 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 164180 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 188149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 188149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 1473 6 None 1 3 Human 7.4 pIC50 = 7.4 Binding
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 1473 6 None 1 3 Human 7.4 pIC50 = 7.4 Binding
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 1473 6 None 1 3 Human 7.4 pIC50 = 7.4 Binding
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 207138 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 139793 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 139793 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 100735 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 100735 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 100735 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 100735 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 206763 0 None -79 2 Human 7.4 pIC50 = 7.4 Binding
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 166750 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 166750 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 210071 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 156864 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
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 156864 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
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 78564 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 78564 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 94548 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 94548 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 145276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 145276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 159649 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 159649 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 209656 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 156351 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
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 156351 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
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 208417 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 212100 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 191748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 191748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 189938 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 189938 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 166681 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 166681 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 96475 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 96475 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 210067 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 209659 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 14873 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 14873 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 78571 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 78571 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 123325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 123325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 211490 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
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 14969 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 14969 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 75156 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 75156 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 14891 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 14891 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 173387 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 173387 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 136033 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 136033 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 211322 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 163753 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 163753 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 299 23 None - 4 Mouse 8.3 pIC50 = 8.3 Binding
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 87638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 87638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 208854 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pIC50 = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pIC50 = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pIC50 = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pIC50 = 7.3 Binding
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 207137 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 118295 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 118295 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 207336 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 207335 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 210420 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 208863 1 None -39 2 Mouse 4.3 pIC50 = 4.3 Binding
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 210077 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 140138 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 140138 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 173237 0 None -79 4 Mouse 4.3 pIC50 = 4.3 Binding
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 173237 0 None -79 4 Mouse 4.3 pIC50 = 4.3 Binding
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 158087 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
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 158087 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
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 210075 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 164081 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 164081 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 157307 0 None - 1 Mouse 6.3 pIC50 = 6.3 Binding
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 157307 0 None - 1 Mouse 6.3 pIC50 = 6.3 Binding
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 212195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 78072 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 78072 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 163810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 163810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 166924 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 166924 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 122044 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 122044 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 163568 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 163568 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 210476 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 211408 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 212061 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 207422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 210806 15 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 210806 15 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 208528 0 None 15 2 Human 8.2 pIC50 = 8.2 Binding
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 210806 15 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 210806 15 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 211604 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 122043 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 122043 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 209659 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 188237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 188237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 211132 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 66857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 66857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 78561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 78561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 78338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 78338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 208863 1 None - 2 Human 7.2 pIC50 = 7.2 Binding
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 139814 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 139814 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 208415 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 207318 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 191644 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 191644 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 210073 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 60484 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 60484 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 159024 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
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 159024 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
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 14861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 14861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 210080 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 168313 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 168313 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 190472 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 190472 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 1473 6 None 1 3 Human 7.2 pIC50 = 7.2 Binding
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 1473 6 None 1 3 Human 7.2 pIC50 = 7.2 Binding
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 1473 6 None 1 3 Human 7.2 pIC50 = 7.2 Binding
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 1473 6 None 1 3 Human 7.1 pIC50 = 7.1 Binding
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 1473 6 None 1 3 Human 7.1 pIC50 = 7.1 Binding
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 1473 6 None 1 3 Human 7.1 pIC50 = 7.1 Binding
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 209659 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 163206 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 163206 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 189512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 189512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 60488 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 60488 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 60486 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 60486 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 140830 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 140830 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pIC50 = 6.1 Binding
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 14870 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 14870 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 207333 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 209081 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 210425 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 121914 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 121914 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 121920 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 121920 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 299 23 None - 4 Mouse 8.1 pIC50 = 8.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 2649 49 None -72 3 Human 8.1 pIC50 = 8.1 Binding
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 209659 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 211000 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 66907 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 66907 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 160192 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 160192 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 75068 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 75068 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 210521 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
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 210485 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 14872 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 14872 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 8308 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 8308 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 121917 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
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 121917 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
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 2649 49 None -72 3 Human 8.0 pIC50 = 8.0 Binding
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 2649 49 None -72 3 Human 8.0 pIC50 = 8.0 Binding
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 2649 49 None -72 3 Human 8.0 pIC50 = 8.0 Binding
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 166302 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 166302 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 123840 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 123840 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 3369 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 3369 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 3369 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 156261 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 156261 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 78569 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 78569 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 60487 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 60487 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 155630 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 155630 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 210078 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 210686 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 139290 0 None -79 3 Mouse 6.0 pIC50 = 6 Binding
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 139290 0 None -79 3 Mouse 6.0 pIC50 = 6 Binding
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 3543 12 None -12 7 Mouse 9.5 pKd = 9.5 Binding
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 3543 12 None -12 7 Mouse 9.5 pKd = 9.5 Binding
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 3543 12 None -12 7 Mouse 9.5 pKd = 9.5 Binding
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 3543 12 None -12 7 Mouse 9.5 pKd = 9.5 Binding
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 10165 0 None -2 2 Human 9.4 pKd = 9.4 Binding
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 10165 0 None -2 2 Human 9.4 pKd = 9.4 Binding
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 208528 0 None 15 2 Human 9.2 pKd = 9.2 Binding
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 206766 0 None -1 2 Human 9.0 pKd = 9 Binding
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 3543 12 None -12 7 Mouse 8.7 pKd = 8.7 Binding
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 3543 12 None -12 7 Mouse 8.7 pKd = 8.7 Binding
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 3543 12 None -12 7 Mouse 8.7 pKd = 8.7 Binding
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 3543 12 None -12 7 Mouse 8.7 pKd = 8.7 Binding
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 207462 0 None -5 2 Human 8.7 pKd = 8.7 Binding
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 120748 0 None -25 2 Mouse 7.0 pKd = 7 Binding
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 120748 0 None -25 2 Mouse 7.0 pKd = 7 Binding
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 210006 0 None -19 2 Mouse 7.0 pKd = 7 Binding
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 120740 0 None -10 2 Mouse 6.0 pKd = 6 Binding
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 120740 0 None -10 2 Mouse 6.0 pKd = 6 Binding
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 120747 0 None -162 2 Mouse 6.9 pKd = 6.9 Binding
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 120747 0 None -162 2 Mouse 6.9 pKd = 6.9 Binding
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 118375 0 None -251 2 Mouse 5.9 pKd = 5.9 Binding
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 118375 0 None -251 2 Mouse 5.9 pKd = 5.9 Binding
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 210001 0 None -7 2 Mouse 5.9 pKd = 5.9 Binding
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 120749 0 None -31 2 Mouse 6.8 pKd = 6.8 Binding
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 120749 0 None -31 2 Mouse 6.8 pKd = 6.8 Binding
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 210007 0 None -50 2 Mouse 6.7 pKd = 6.7 Binding
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 118376 0 None -398 2 Mouse 5.7 pKd = 5.7 Binding
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 118376 0 None -398 2 Mouse 5.7 pKd = 5.7 Binding
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 210005 0 None -6 2 Mouse 7.6 pKd = 7.6 Binding
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 206764 0 None 12 2 Human 7.6 pKd = 7.6 Binding
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 120745 0 None -158 2 Mouse 5.6 pKd = 5.6 Binding
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 120745 0 None -158 2 Mouse 5.6 pKd = 5.6 Binding
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 206763 0 None -79 2 Human 6.5 pKd = 6.5 Binding
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 210002 1 None -31 3 Mouse 6.4 pKd = 6.4 Binding
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 206765 0 None -19 2 Human 6.4 pKd = 6.4 Binding
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 118372 0 None -251 2 Mouse 5.4 pKd = 5.4 Binding
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 118372 0 None -251 2 Mouse 5.4 pKd = 5.4 Binding
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 212121 0 None -25 2 Human 8.3 pKd = 8.3 Binding
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 207462 0 None -5 2 Human 8.3 pKd = 8.3 Binding
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 206767 0 None -5 2 Human 8.2 pKd = 8.2 Binding
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 209998 0 None -3 2 Mouse 6.2 pKd = 6.2 Binding
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 209999 0 None -10 2 Mouse 6.2 pKd = 6.2 Binding
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 210003 0 None -3 2 Mouse 6.2 pKd = 6.2 Binding
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 210010 0 None - 1 Mouse 6.2 pKd = 6.2 Binding
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 206762 0 None -63 2 Human 6.2 pKd = 6.2 Binding
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 120739 0 None -50 2 Mouse 6.1 pKd = 6.1 Binding
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 120739 0 None -50 2 Mouse 6.1 pKd = 6.1 Binding
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 209997 0 None -2 2 Mouse 6.1 pKd = 6.1 Binding
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 210009 0 None - 1 Mouse 6.1 pKd = 6.1 Binding
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 208527 0 None -316 2 Human 6.1 pKd = 6.1 Binding
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 181142 0 None -1 2 Human 10.7 pKi = 10.7 Binding
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 181142 0 None -1 2 Human 10.7 pKi = 10.7 Binding
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 181142 0 None -1 2 Human 10.7 pKi = 10.7 Binding
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 181142 0 None -1 2 Human 10.7 pKi = 10.7 Binding
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 182471 0 None -1 2 Human 10.5 pKi = 10.5 Binding
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 182471 0 None -1 2 Human 10.5 pKi = 10.5 Binding
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 182471 0 None -1 2 Human 10.5 pKi = 10.5 Binding
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 182471 0 None -1 2 Human 10.5 pKi = 10.5 Binding
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 182871 0 None -2 2 Human 10.5 pKi = 10.5 Binding
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 182871 0 None -2 2 Human 10.5 pKi = 10.5 Binding
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 182871 0 None -2 2 Human 10.5 pKi = 10.5 Binding
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 182871 0 None -2 2 Human 10.5 pKi = 10.5 Binding
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 211403 0 None -1 4 Human 10.0 pKi = 10.0 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 3543 12 None -5 7 Human 9.9 pKi = 9.9 Binding
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 182476 0 None -8 2 Human 9.9 pKi = 9.9 Binding
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 182476 0 None -8 2 Human 9.9 pKi = 9.9 Binding
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 182476 0 None -8 2 Human 9.9 pKi = 9.9 Binding
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 182476 0 None -8 2 Human 9.9 pKi = 9.9 Binding
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 208226 0 None 1 3 Human 9.7 pKi = 9.7 Binding
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 212168 0 None -3 3 Human 9.6 pKi = 9.6 Binding
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 211428 0 None -2 4 Human 9.6 pKi = 9.6 Binding
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 182008 0 None -15 2 Human 9.5 pKi = 9.5 Binding
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 182008 0 None -15 2 Human 9.5 pKi = 9.5 Binding
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 182008 0 None -15 2 Human 9.5 pKi = 9.5 Binding
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 182008 0 None -15 2 Human 9.5 pKi = 9.5 Binding
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 182542 0 None -13 2 Human 9.5 pKi = 9.5 Binding
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 182542 0 None -13 2 Human 9.5 pKi = 9.5 Binding
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 182542 0 None -13 2 Human 9.5 pKi = 9.5 Binding
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 182542 0 None -13 2 Human 9.5 pKi = 9.5 Binding
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 182289 0 None -13 2 Human 9.4 pKi = 9.4 Binding
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 182289 0 None -13 2 Human 9.4 pKi = 9.4 Binding
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 182289 0 None -13 2 Human 9.4 pKi = 9.4 Binding
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 182289 0 None -13 2 Human 9.4 pKi = 9.4 Binding
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 182439 0 None -18 2 Human 9.4 pKi = 9.4 Binding
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 182439 0 None -18 2 Human 9.4 pKi = 9.4 Binding
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 182439 0 None -18 2 Human 9.4 pKi = 9.4 Binding
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 182439 0 None -18 2 Human 9.4 pKi = 9.4 Binding
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 189706 0 None 1 2 Human 9.2 pKi = 9.2 Binding
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 189706 0 None 1 2 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.2 pKi = 9.2 Binding
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 182975 0 None -19 2 Human 9.2 pKi = 9.2 Binding
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 182975 0 None -19 2 Human 9.2 pKi = 9.2 Binding
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 182975 0 None -19 2 Human 9.2 pKi = 9.2 Binding
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 182975 0 None -19 2 Human 9.2 pKi = 9.2 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 299 23 None -2 4 Human 9.1 pKi = 9.1 Binding
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 208222 0 None 1 3 Human 9.1 pKi = 9.1 Binding
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 210604 0 None -10 3 Human 9.0 pKi = 9.0 Binding
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 79541 0 None -2 3 Human 9.0 pKi = 9 Binding
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 79541 0 None -2 3 Human 9.0 pKi = 9 Binding
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 138740 0 None -1 3 Human 9.0 pKi = 9 Binding
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 138740 0 None -1 3 Human 9.0 pKi = 9 Binding
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 141056 0 None -2 3 Human 9.0 pKi = 9.0 Binding
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 141056 0 None -2 3 Human 9.0 pKi = 9.0 Binding
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 208056 0 None -1 3 Human 8.9 pKi = 8.9 Binding
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 208961 0 None -6 4 Human 8.8 pKi = 8.8 Binding
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 181714 0 None -10 2 Human 8.0 pKi = 8 Binding
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 181714 0 None -10 2 Human 8.0 pKi = 8 Binding
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 181714 0 None -10 2 Human 8.0 pKi = 8 Binding
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 181714 0 None -10 2 Human 8.0 pKi = 8 Binding
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 189731 0 None -24 3 Human 8.0 pKi = 8.0 Binding
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 189731 0 None -24 3 Human 8.0 pKi = 8.0 Binding
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 211254 17 None -12 4 Human 8.0 pKi = 8.0 Binding
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 211254 17 None -12 4 Human 8.0 pKi = 8.0 Binding
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 190718 0 None -15 3 Human 8.0 pKi = 8.0 Binding
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 190718 0 None -15 3 Human 8.0 pKi = 8.0 Binding
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 120748 0 None -25 2 Mouse 7.0 pKi = 7 Binding
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 120748 0 None -25 2 Mouse 7.0 pKi = 7 Binding
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 210006 0 None -19 2 Mouse 7.0 pKi = 7 Binding
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 213345 0 None -26 3 Human 7.0 pKi = 7 Binding
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 68299 0 None -416 2 Human 6.0 pKi = 6 Binding
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 68299 0 None -416 2 Human 6.0 pKi = 6 Binding
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 66490 0 None -58 4 Human 6.0 pKi = 6 Binding
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 66490 0 None -58 4 Human 6.0 pKi = 6 Binding
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 120740 0 None -10 2 Mouse 6.0 pKi = 6 Binding
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 120740 0 None -10 2 Mouse 6.0 pKi = 6 Binding
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 89611 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-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 89611 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-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 213704 0 None -707 3 Human 7.0 pKi = 7.0 Binding
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 213511 0 None -75 3 Human 7.0 pKi = 7.0 Binding
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 135150 0 None -3 2 Human 5.0 pKi = 5.0 Binding
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 135150 0 None -3 2 Human 5.0 pKi = 5.0 Binding
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
176 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
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 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
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 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
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 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
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 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
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 76449 0 None -85 4 Human 8.0 pKi = 8.0 Binding
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 76449 0 None -85 4 Human 8.0 pKi = 8.0 Binding
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 76449 0 None -85 4 Human 8.0 pKi = 8.0 Binding
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 76449 0 None -85 4 Human 8.0 pKi = 8.0 Binding
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 190083 0 None -17 3 Human 7.9 pKi = 7.9 Binding
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 190083 0 None -17 3 Human 7.9 pKi = 7.9 Binding
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 189839 0 None -14 3 Human 7.9 pKi = 7.9 Binding
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 189839 0 None -14 3 Human 7.9 pKi = 7.9 Binding
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 105680 0 None 6 3 Human 7.0 pKi = 7.0 Binding
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 105680 0 None 6 3 Human 7.0 pKi = 7.0 Binding
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 162818 0 None -18 3 Human 7.0 pKi = 7.0 Binding
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 162818 0 None -18 3 Human 7.0 pKi = 7.0 Binding
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 190807 0 None -3 4 Human 7.0 pKi = 7.0 Binding
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 190807 0 None -3 4 Human 7.0 pKi = 7.0 Binding
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 152509 0 None -575 3 Human 6.0 pKi = 6.0 Binding
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 152509 0 None -575 3 Human 6.0 pKi = 6.0 Binding
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 207441 0 None -31 3 Human 6.0 pKi = 6.0 Binding
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 67032 0 None -131 4 Human 6.0 pKi = 6.0 Binding
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 67032 0 None -131 4 Human 6.0 pKi = 6.0 Binding
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 124902 1 None -316 4 Human 6.0 pKi = 6.0 Binding
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 124902 1 None -316 4 Human 6.0 pKi = 6.0 Binding
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 88605 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 88605 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 124670 0 None -4 2 Human 6.0 pKi = 6.0 Binding
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 124670 0 None -4 2 Human 6.0 pKi = 6.0 Binding
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 10203 0 None -2 2 Human 5.0 pKi = 5.0 Binding
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 10203 0 None -2 2 Human 5.0 pKi = 5.0 Binding
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 79473 0 None -5 3 Human 5.9 pKi = 5.9 Binding
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 79473 0 None -5 3 Human 5.9 pKi = 5.9 Binding
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 212808 0 None -75 3 Human 5.9 pKi = 5.9 Binding
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 137940 0 None -91 3 Human 6.9 pKi = 6.9 Binding
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 137940 0 None -91 3 Human 6.9 pKi = 6.9 Binding
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 57919 0 None -10 4 Human 5.9 pKi = 5.9 Binding
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 57919 0 None -10 4 Human 5.9 pKi = 5.9 Binding
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 79334 0 None -93 3 Human 5.9 pKi = 5.9 Binding
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 79334 0 None -93 3 Human 5.9 pKi = 5.9 Binding
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 79334 0 None -93 3 Human 5.9 pKi = 5.9 Binding
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 79334 0 None -93 3 Human 5.9 pKi = 5.9 Binding
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 208225 0 None -2 2 Human 7.9 pKi = 7.9 Binding
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 167493 0 None 7 3 Human 7.9 pKi = 7.9 Binding
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 167493 0 None 7 3 Human 7.9 pKi = 7.9 Binding
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 16151 0 None -181 3 Human 6.9 pKi = 6.9 Binding
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 16151 0 None -181 3 Human 6.9 pKi = 6.9 Binding
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 79310 0 None -63 3 Human 5.9 pKi = 5.9 Binding
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 79310 0 None -63 3 Human 5.9 pKi = 5.9 Binding
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 79310 0 None -63 3 Human 5.9 pKi = 5.9 Binding
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 79310 0 None -63 3 Human 5.9 pKi = 5.9 Binding
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 78624 0 None -1 4 Human 5.9 pKi = 5.9 Binding
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 78624 0 None -1 4 Human 5.9 pKi = 5.9 Binding
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 78629 0 None -4 4 Human 5.9 pKi = 5.9 Binding
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 78629 0 None -4 4 Human 5.9 pKi = 5.9 Binding
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 88822 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 88822 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89182 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89182 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89306 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89306 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 154176 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 154176 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 76573 0 None -707 4 Human 6.9 pKi = 6.9 Binding
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 76573 0 None -707 4 Human 6.9 pKi = 6.9 Binding
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 76573 0 None -707 4 Human 6.9 pKi = 6.9 Binding
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 76573 0 None -707 4 Human 6.9 pKi = 6.9 Binding
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 191877 0 None -190 3 Human 4.9 pKi = 4.9 Binding
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 191877 0 None -190 3 Human 4.9 pKi = 4.9 Binding
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 139274 0 None -4 3 Human 5.9 pKi = 5.9 Binding
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 139274 0 None -4 3 Human 5.9 pKi = 5.9 Binding
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 3747 37 None -70 4 Human 6.9 pKi = 6.9 Binding
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 3747 37 None -70 4 Human 6.9 pKi = 6.9 Binding
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 3747 37 None -70 4 Human 6.9 pKi = 6.9 Binding
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 77712 0 None -10 3 Human 5.9 pKi = 5.9 Binding
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 77712 0 None -10 3 Human 5.9 pKi = 5.9 Binding
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 188262 0 None -23 3 Human 6.9 pKi = 6.9 Binding
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 188262 0 None -23 3 Human 6.9 pKi = 6.9 Binding
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 188235 0 None -32 3 Human 6.9 pKi = 6.9 Binding
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 188235 0 None -32 3 Human 6.9 pKi = 6.9 Binding
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 190081 0 None -128 3 Human 4.9 pKi = 4.9 Binding
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 190081 0 None -128 3 Human 4.9 pKi = 4.9 Binding
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 76575 0 None -50 4 Human 7.9 pKi = 7.9 Binding
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 76575 0 None -50 4 Human 7.9 pKi = 7.9 Binding
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 76575 0 None -50 4 Human 7.9 pKi = 7.9 Binding
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 76575 0 None -50 4 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 3536 18 None -3 5 Human 7.9 pKi = 7.9 Binding
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 189671 0 None -33 3 Human 7.9 pKi = 7.9 Binding
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 189671 0 None -33 3 Human 7.9 pKi = 7.9 Binding
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 167409 0 None -1 2 Human 7.9 pKi = 7.9 Binding
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 167409 0 None -1 2 Human 7.9 pKi = 7.9 Binding
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 191568 0 None -56 3 Human 7.9 pKi = 7.9 Binding
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 191568 0 None -56 3 Human 7.9 pKi = 7.9 Binding
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 106529 0 None -3 3 Human 6.9 pKi = 6.9 Binding
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 106529 0 None -3 3 Human 6.9 pKi = 6.9 Binding
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 120747 0 None -162 2 Mouse 6.9 pKi = 6.9 Binding
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 120747 0 None -162 2 Mouse 6.9 pKi = 6.9 Binding
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 87326 0 None -38 4 Human 6.9 pKi = 6.9 Binding
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 87326 0 None -38 4 Human 6.9 pKi = 6.9 Binding
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 68822 0 None -288 3 Human 5.9 pKi = 5.9 Binding
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 68822 0 None -288 3 Human 5.9 pKi = 5.9 Binding
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 154899 0 None -275 4 Human 5.9 pKi = 5.9 Binding
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 154899 0 None -275 4 Human 5.9 pKi = 5.9 Binding
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 210000 0 None -8 2 Mouse 5.9 pKi = 5.9 Binding
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 79679 0 None -51 4 Human 5.9 pKi = 5.9 Binding
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 79679 0 None -51 4 Human 5.9 pKi = 5.9 Binding
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 79679 0 None -51 4 Human 5.9 pKi = 5.9 Binding
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 79679 0 None -51 4 Human 5.9 pKi = 5.9 Binding
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 88272 0 None -3 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 88272 0 None -3 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89598 0 None -8 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89598 0 None -8 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 147627 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 147627 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 191048 0 None -190 3 Human 4.9 pKi = 4.9 Binding
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 191048 0 None -190 3 Human 4.9 pKi = 4.9 Binding
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 212917 0 None -16 3 Human 6.9 pKi = 6.9 Binding
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 502 77 None -147 41 Human 4.9 pKi = 4.9 Binding
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
249 502 77 None -147 41 Human 4.9 pKi = 4.9 Binding
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 502 77 None -147 41 Human 4.9 pKi = 4.9 Binding
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 502 77 None -147 41 Human 4.9 pKi = 4.9 Binding
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 502 77 None -147 41 Human 4.9 pKi = 4.9 Binding
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 70854 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 70854 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 211494 0 None -8 3 Human 7.9 pKi = 7.9 Binding
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 208938 0 None -8 3 Human 6.9 pKi = 6.9 Binding
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 167640 0 None 4 3 Human 6.9 pKi = 6.9 Binding
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 167640 0 None 4 3 Human 6.9 pKi = 6.9 Binding
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 105484 0 None -12 3 Human 6.9 pKi = 6.9 Binding
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 105484 0 None -12 3 Human 6.9 pKi = 6.9 Binding
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 208223 0 None -1 3 Human 5.9 pKi = 5.9 Binding
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 89494 0 None -165 3 Human 5.9 pKi = 5.9 Binding
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 89494 0 None -165 3 Human 5.9 pKi = 5.9 Binding
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 168154 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 168154 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 66487 0 None -93 4 Human 5.9 pKi = 5.9 Binding
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 66487 0 None -93 4 Human 5.9 pKi = 5.9 Binding
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 66536 0 None -100 4 Human 5.9 pKi = 5.9 Binding
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 66536 0 None -100 4 Human 5.9 pKi = 5.9 Binding
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 79736 0 None -12 3 Human 5.9 pKi = 5.9 Binding
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 79736 0 None -12 3 Human 5.9 pKi = 5.9 Binding
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 76421 0 None -14 4 Human 5.9 pKi = 5.9 Binding
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 76421 0 None -14 4 Human 5.9 pKi = 5.9 Binding
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 66490 0 None -58 4 Human 5.9 pKi = 5.9 Binding
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 66490 0 None -58 4 Human 5.9 pKi = 5.9 Binding
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 10090 0 None -4 4 Human 4.9 pKi = 4.9 Binding
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 10090 0 None -4 4 Human 4.9 pKi = 4.9 Binding
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 89307 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 89307 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 148161 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 148161 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 152209 0 None -7 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 152209 0 None -7 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-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 176445 0 None -23 3 Human 6.8 pKi = 6.8 Binding
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 176445 0 None -23 3 Human 6.8 pKi = 6.8 Binding
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 212945 0 None -30 3 Human 6.8 pKi = 6.8 Binding
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 123498 0 None -2 2 Human 5.8 pKi = 5.8 Binding
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 123498 0 None -2 2 Human 5.8 pKi = 5.8 Binding
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 138144 0 None -2 3 Human 5.8 pKi = 5.8 Binding
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 138144 0 None -2 3 Human 5.8 pKi = 5.8 Binding
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 208221 0 None -10 3 Human 7.8 pKi = 7.8 Binding
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 182256 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 182256 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 182256 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 182256 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 155330 0 None -5 3 Human 7.8 pKi = 7.8 Binding
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 155330 0 None -5 3 Human 7.8 pKi = 7.8 Binding
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 210938 0 None -56 4 Human 7.8 pKi = 7.8 Binding
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 210998 0 None -12 3 Human 6.8 pKi = 6.8 Binding
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 212011 0 None 1 2 Human 6.8 pKi = 6.8 Binding
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 16403 0 None -301 3 Human 6.8 pKi = 6.8 Binding
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 16403 0 None -301 3 Human 6.8 pKi = 6.8 Binding
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 112847 0 None -13 3 Human 5.8 pKi = 5.8 Binding
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 112847 0 None -13 3 Human 5.8 pKi = 5.8 Binding
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 66096 0 None -1 4 Human 4.8 pKi = 4.8 Binding
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 66096 0 None -1 4 Human 4.8 pKi = 4.8 Binding
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 88086 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88086 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89474 0 None -15 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89474 0 None -15 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 32474 12 None -45 10 Human 4.8 pKi = 4.8 Binding
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 32474 12 None -45 10 Human 4.8 pKi = 4.8 Binding
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 32474 12 None -45 10 Human 4.8 pKi = 4.8 Binding
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 138486 0 None -34 3 Human 4.8 pKi = 4.8 Binding
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 138486 0 None -34 3 Human 4.8 pKi = 4.8 Binding
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 138410 0 None -2 3 Human 6.8 pKi = 6.8 Binding
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 138410 0 None -2 3 Human 6.8 pKi = 6.8 Binding
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 171978 0 None -30 3 Human 6.8 pKi = 6.8 Binding
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 171978 0 None -30 3 Human 6.8 pKi = 6.8 Binding
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 79867 0 None -5 3 Human 6.8 pKi = 6.8 Binding
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 79867 0 None -5 3 Human 6.8 pKi = 6.8 Binding
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 189492 0 None -9 3 Human 7.8 pKi = 7.8 Binding
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 189492 0 None -9 3 Human 7.8 pKi = 7.8 Binding
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 2649 49 None -72 3 Human 7.8 pKi = 7.8 Binding
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 2649 49 None -72 3 Human 7.8 pKi = 7.8 Binding
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 2649 49 None -72 3 Human 7.8 pKi = 7.8 Binding
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 111081 0 None -2 3 Human 6.8 pKi = 6.8 Binding
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 111081 0 None -2 3 Human 6.8 pKi = 6.8 Binding
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 120749 0 None -31 2 Mouse 6.8 pKi = 6.8 Binding
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 120749 0 None -31 2 Mouse 6.8 pKi = 6.8 Binding
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 178069 0 None -144 3 Human 6.8 pKi = 6.8 Binding
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 178069 0 None -144 3 Human 6.8 pKi = 6.8 Binding
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 211609 0 None -7 3 Human 5.8 pKi = 5.8 Binding
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 145528 0 None -138 4 Human 5.8 pKi = 5.8 Binding
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 145528 0 None -138 4 Human 5.8 pKi = 5.8 Binding
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 123820 0 None -512 2 Human 5.8 pKi = 5.8 Binding
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 123820 0 None -512 2 Human 5.8 pKi = 5.8 Binding
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 76576 0 None -6 3 Human 5.8 pKi = 5.8 Binding
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 76576 0 None -6 3 Human 5.8 pKi = 5.8 Binding
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 76576 0 None -6 3 Human 5.8 pKi = 5.8 Binding
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 88870 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88870 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89002 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89002 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89596 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89596 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 166793 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 166793 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 168334 0 None -213 4 Human 4.8 pKi = 4.8 Binding
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 168334 0 None -213 4 Human 4.8 pKi = 4.8 Binding
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 205195 91 None -54 34 Human 4.8 pKi = 4.8 Binding
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 205195 91 None -54 34 Human 4.8 pKi = 4.8 Binding
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 205195 91 None -54 34 Human 4.8 pKi = 4.8 Binding
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 140056 0 None -67 3 Human 5.8 pKi = 5.8 Binding
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 140056 0 None -67 3 Human 5.8 pKi = 5.8 Binding
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 168890 0 None -13 3 Human 6.8 pKi = 6.8 Binding
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 168890 0 None -13 3 Human 6.8 pKi = 6.8 Binding
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 211616 0 None -60 4 Human 6.8 pKi = 6.8 Binding
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 207698 0 None 1 3 Human 6.8 pKi = 6.8 Binding
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 189660 0 None -1 4 Human 6.8 pKi = 6.8 Binding
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 189660 0 None -1 4 Human 6.8 pKi = 6.8 Binding
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 79961 0 None -13 3 Human 7.8 pKi = 7.8 Binding
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 79961 0 None -13 3 Human 7.8 pKi = 7.8 Binding
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 155534 0 None -8 3 Human 6.8 pKi = 6.8 Binding
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 155534 0 None -8 3 Human 6.8 pKi = 6.8 Binding
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 172033 0 None -12 3 Human 6.8 pKi = 6.8 Binding
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 172033 0 None -12 3 Human 6.8 pKi = 6.8 Binding
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 188850 0 None -208 3 Human 5.8 pKi = 5.8 Binding
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 188850 0 None -208 3 Human 5.8 pKi = 5.8 Binding
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 89008 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-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 89008 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-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 88540 0 None -11 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88540 0 None -11 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89166 0 None -14 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89166 0 None -14 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 154134 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 154134 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 74085 0 None -16 3 Human 5.8 pKi = 5.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 3690 75 None -56 35 Human 4.8 pKi = 4.8 Binding
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 212608 0 None -1348 3 Human 5.8 pKi = 5.8 Binding
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 159170 0 None -63 3 Human 4.8 pKi = 4.8 Binding
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 159170 0 None -63 3 Human 4.8 pKi = 4.8 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 2649 49 None -72 3 Human 7.7 pKi = 7.7 Binding
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 147650 0 None -251 7 Mouse 6.8 pKi = 6.8 Binding
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 147650 0 None -251 7 Mouse 6.8 pKi = 6.8 Binding
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 124254 0 None -43 3 Human 5.8 pKi = 5.8 Binding
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 124254 0 None -43 3 Human 5.8 pKi = 5.8 Binding
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 127985 0 None -158 4 Human 5.8 pKi = 5.8 Binding
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 127985 0 None -158 4 Human 5.8 pKi = 5.8 Binding
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 168478 0 None -323 4 Human 5.8 pKi = 5.8 Binding
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 168478 0 None -323 4 Human 5.8 pKi = 5.8 Binding
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 88085 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 88085 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89483 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 89483 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-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 96602 0 None -13 4 Human 4.8 pKi = 4.8 Binding
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 96602 0 None -13 4 Human 4.8 pKi = 4.8 Binding
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 76169 0 None -85 3 Human 4.7 pKi = 4.7 Binding
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 76169 0 None -85 3 Human 4.7 pKi = 4.7 Binding
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 176151 0 None -2 3 Human 5.7 pKi = 5.7 Binding
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 176151 0 None -2 3 Human 5.7 pKi = 5.7 Binding
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 189362 0 None -14 3 Human 7.7 pKi = 7.7 Binding
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 189362 0 None -14 3 Human 7.7 pKi = 7.7 Binding
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 210901 0 None -44 3 Human 6.7 pKi = 6.7 Binding
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 187469 0 None -54 7 Mouse 6.7 pKi = 6.7 Binding
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 187469 0 None -54 7 Mouse 6.7 pKi = 6.7 Binding
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 155305 0 None -74 3 Mouse 6.7 pKi = 6.7 Binding
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 155305 0 None -74 3 Mouse 6.7 pKi = 6.7 Binding
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 178091 0 None -56 3 Human 6.7 pKi = 6.7 Binding
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 178091 0 None -56 3 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 64612 0 None -301 2 Human 5.7 pKi = 5.7 Binding
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 64612 0 None -301 2 Human 5.7 pKi = 5.7 Binding
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 214119 0 None -11 3 Human 5.7 pKi = 5.7 Binding
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 143281 0 None -43 3 Human 5.7 pKi = 5.7 Binding
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 143281 0 None -43 3 Human 5.7 pKi = 5.7 Binding
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 139713 0 None -331 4 Human 5.7 pKi = 5.7 Binding
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 139713 0 None -331 4 Human 5.7 pKi = 5.7 Binding
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 143281 0 None -43 3 Human 5.7 pKi = 5.7 Binding
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 143281 0 None -43 3 Human 5.7 pKi = 5.7 Binding
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 88169 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 145772 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 145772 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 147084 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 147084 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 147370 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 147370 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 78740 0 None -12 4 Human 4.7 pKi = 4.7 Binding
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 78740 0 None -12 4 Human 4.7 pKi = 4.7 Binding
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 79657 0 None -11 3 Human 4.7 pKi = 4.7 Binding
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 79657 0 None -11 3 Human 4.7 pKi = 4.7 Binding
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 155985 0 None -288 3 Human 5.7 pKi = 5.7 Binding
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 155985 0 None -288 3 Human 5.7 pKi = 5.7 Binding
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 79818 0 None -138 3 Human 5.7 pKi = 5.7 Binding
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 79818 0 None -138 3 Human 5.7 pKi = 5.7 Binding
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 176498 0 None -11 4 Human 4.7 pKi = 4.7 Binding
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 176498 0 None -11 4 Human 4.7 pKi = 4.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 712 26 None -23 4 Human 6.7 pKi = 6.7 Binding
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 76568 0 None -5 4 Human 8.7 pKi = 8.7 Binding
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 76568 0 None -5 4 Human 8.7 pKi = 8.7 Binding
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 76567 0 None -20 4 Human 8.6 pKi = 8.6 Binding
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 76567 0 None -20 4 Human 8.6 pKi = 8.6 Binding
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 210988 0 None -6 3 Human 8.6 pKi = 8.6 Binding
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 208123 0 None -9 3 Human 7.7 pKi = 7.7 Binding
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 209615 0 None -70 3 Human 7.7 pKi = 7.7 Binding
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 205452 0 None -5 3 Human 7.7 pKi = 7.7 Binding
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 205452 0 None -5 3 Human 7.7 pKi = 7.7 Binding
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 191028 0 None -6 3 Human 7.7 pKi = 7.7 Binding
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 191028 0 None -6 3 Human 7.7 pKi = 7.7 Binding
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 210007 0 None -50 2 Mouse 6.7 pKi = 6.7 Binding
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 192771 0 None -48 3 Human 6.7 pKi = 6.7 Binding
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 192771 0 None -48 3 Human 6.7 pKi = 6.7 Binding
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 122428 0 None -309 4 Human 5.7 pKi = 5.7 Binding
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 122428 0 None -309 4 Human 5.7 pKi = 5.7 Binding
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 88977 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88977 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88996 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88996 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 154176 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 154176 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 177895 0 None -25 3 Human 6.7 pKi = 6.7 Binding
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 177895 0 None -25 3 Human 6.7 pKi = 6.7 Binding
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 80686 0 None -38 3 Human 6.7 pKi = 6.7 Binding
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 80686 0 None -38 3 Human 6.7 pKi = 6.7 Binding
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 188117 0 None -34 3 Human 6.7 pKi = 6.7 Binding
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 188117 0 None -34 3 Human 6.7 pKi = 6.7 Binding
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 111889 0 None -4 3 Human 6.7 pKi = 6.7 Binding
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 111889 0 None -4 3 Human 6.7 pKi = 6.7 Binding
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 151410 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-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 151410 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 168356 0 None -3 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 168356 0 None -3 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 906 64 None -186 72 Human 4.7 pKi = 4.7 Binding
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
621 906 64 None -186 72 Human 4.7 pKi = 4.7 Binding
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
83 906 64 None -186 72 Human 4.7 pKi = 4.7 Binding
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 906 64 None -186 72 Human 4.7 pKi = 4.7 Binding
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 906 64 None -186 72 Human 4.7 pKi = 4.7 Binding
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 171931 0 None -6 3 Human 6.7 pKi = 6.7 Binding
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 171931 0 None -6 3 Human 6.7 pKi = 6.7 Binding
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 137021 0 None -4 3 Human 6.7 pKi = 6.7 Binding
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 137021 0 None -4 3 Human 6.7 pKi = 6.7 Binding
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 207440 0 None -21 4 Human 7.7 pKi = 7.7 Binding
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 178070 0 None -275 3 Human 6.7 pKi = 6.7 Binding
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 178070 0 None -275 3 Human 6.7 pKi = 6.7 Binding
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 65835 0 None -123 4 Human 5.7 pKi = 5.7 Binding
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 65835 0 None -123 4 Human 5.7 pKi = 5.7 Binding
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 88089 0 None -7 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88089 0 None -7 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88995 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 88995 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89071 0 None -16 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89071 0 None -16 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89313 0 None -27 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89313 0 None -27 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89591 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89591 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-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 190652 0 None -3 4 Human 6.7 pKi = 6.7 Binding
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 190652 0 None -3 4 Human 6.7 pKi = 6.7 Binding
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 141424 0 None -17 3 Human 4.7 pKi = 4.7 Binding
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 141424 0 None -17 3 Human 4.7 pKi = 4.7 Binding
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 141424 0 None -17 3 Human 4.7 pKi = 4.7 Binding
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 141424 0 None -17 3 Human 4.7 pKi = 4.7 Binding
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 139593 0 None -2 3 Human 7.6 pKi = 7.6 Binding
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 139593 0 None -2 3 Human 7.6 pKi = 7.6 Binding
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 190645 0 None -11 3 Human 7.6 pKi = 7.6 Binding
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 190645 0 None -11 3 Human 7.6 pKi = 7.6 Binding
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 110945 0 None -3 3 Human 6.6 pKi = 6.6 Binding
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 110945 0 None -3 3 Human 6.6 pKi = 6.6 Binding
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 91127 0 None -81 3 Human 6.6 pKi = 6.6 Binding
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 91127 0 None -81 3 Human 6.6 pKi = 6.6 Binding
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 91127 0 None -81 3 Human 6.6 pKi = 6.6 Binding
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 91127 0 None -81 3 Human 6.6 pKi = 6.6 Binding
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 66560 0 None -63 3 Human 5.6 pKi = 5.6 Binding
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 66560 0 None -63 3 Human 5.6 pKi = 5.6 Binding
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 176243 0 None -95 3 Human 5.6 pKi = 5.6 Binding
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 176243 0 None -95 3 Human 5.6 pKi = 5.6 Binding
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 3747 37 None -70 4 Human 5.6 pKi = 5.6 Binding
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 3747 37 None -70 4 Human 5.6 pKi = 5.6 Binding
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 3747 37 None -70 4 Human 5.6 pKi = 5.6 Binding
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 126244 0 None -85 4 Human 5.6 pKi = 5.6 Binding
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 126244 0 None -85 4 Human 5.6 pKi = 5.6 Binding
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 97392 0 None -100 2 Human 5.6 pKi = 5.6 Binding
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 97392 0 None -100 2 Human 5.6 pKi = 5.6 Binding
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 66830 0 None -181 3 Human 5.6 pKi = 5.6 Binding
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 66830 0 None -181 3 Human 5.6 pKi = 5.6 Binding
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 88097 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88097 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88529 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88529 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89313 0 None -27 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89313 0 None -27 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 161222 0 None -20 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 161222 0 None -20 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 158282 0 None -64 3 Human 4.6 pKi = 4.6 Binding
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 158282 0 None -64 3 Human 4.6 pKi = 4.6 Binding
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 79386 0 None -41 3 Human 6.6 pKi = 6.6 Binding
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 79386 0 None -41 3 Human 6.6 pKi = 6.6 Binding
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 117444 0 None 11 3 Human 7.6 pKi = 7.6 Binding
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 117444 0 None 11 3 Human 7.6 pKi = 7.6 Binding
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 208853 0 None -1 3 Human 6.6 pKi = 6.6 Binding
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 16151 0 None -181 3 Human 6.6 pKi = 6.6 Binding
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 16151 0 None -181 3 Human 6.6 pKi = 6.6 Binding
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 147650 0 None -338 7 Rat 6.6 pKi = 6.6 Binding
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 147650 0 None -338 7 Rat 6.6 pKi = 6.6 Binding
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 126943 0 None -457 3 Human 5.6 pKi = 5.6 Binding
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 126943 0 None -457 3 Human 5.6 pKi = 5.6 Binding
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 126305 0 None -199 4 Human 5.6 pKi = 5.6 Binding
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 126305 0 None -199 4 Human 5.6 pKi = 5.6 Binding
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 88132 0 None -11 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88132 0 None -11 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88183 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88183 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88745 0 None -19 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88745 0 None -19 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 145433 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 145433 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 152476 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 152476 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 140755 0 None -10 3 Human 5.6 pKi = 5.6 Binding
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 140755 0 None -10 3 Human 5.6 pKi = 5.6 Binding
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 69181 0 None -2 2 Human 5.6 pKi = 5.6 Binding
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 69181 0 None -2 2 Human 5.6 pKi = 5.6 Binding
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 155559 0 None -50 3 Human 4.6 pKi = 4.6 Binding
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 155559 0 None -50 3 Human 4.6 pKi = 4.6 Binding
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 155675 0 None -23 3 Human 4.6 pKi = 4.6 Binding
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 155675 0 None -23 3 Human 4.6 pKi = 4.6 Binding
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 169893 0 None -114 3 Human 4.6 pKi = 4.6 Binding
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 169893 0 None -114 3 Human 4.6 pKi = 4.6 Binding
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 208125 0 None -16 3 Human 7.6 pKi = 7.6 Binding
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 210005 0 None -6 2 Mouse 7.6 pKi = 7.6 Binding
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 69777 0 None -1 2 Human 6.6 pKi = 6.6 Binding
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 69777 0 None -1 2 Human 6.6 pKi = 6.6 Binding
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 66546 0 None -95 4 Human 5.6 pKi = 5.6 Binding
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 66546 0 None -95 4 Human 5.6 pKi = 5.6 Binding
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 178463 0 None -38 3 Human 5.6 pKi = 5.6 Binding
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 178463 0 None -38 3 Human 5.6 pKi = 5.6 Binding
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 120745 0 None -158 2 Mouse 5.6 pKi = 5.6 Binding
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 120745 0 None -158 2 Mouse 5.6 pKi = 5.6 Binding
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 88182 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88182 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89160 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89160 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89305 0 None -17 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89305 0 None -17 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 149019 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 149019 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 152476 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 152476 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 154177 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 154177 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 133093 0 None -8 2 Human 6.6 pKi = 6.6 Binding
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 133093 0 None -8 2 Human 6.6 pKi = 6.6 Binding
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 138988 0 None -40 3 Human 7.6 pKi = 7.6 Binding
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 138988 0 None -40 3 Human 7.6 pKi = 7.6 Binding
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 190786 0 None -16 3 Human 7.6 pKi = 7.6 Binding
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 190786 0 None -16 3 Human 7.6 pKi = 7.6 Binding
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 97476 0 None -223 3 Human 6.6 pKi = 6.6 Binding
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 97476 0 None -223 3 Human 6.6 pKi = 6.6 Binding
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 106668 0 None -8 3 Human 6.6 pKi = 6.6 Binding
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 106668 0 None -8 3 Human 6.6 pKi = 6.6 Binding
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 88173 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88173 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88737 0 None -3 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88737 0 None -3 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89085 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89085 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 148072 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 148072 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 178124 0 None -42 3 Human 4.6 pKi = 4.6 Binding
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 178124 0 None -42 3 Human 4.6 pKi = 4.6 Binding
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 212623 0 None -181 3 Human 6.6 pKi = 6.6 Binding
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 76574 0 None -338 4 Human 7.6 pKi = 7.6 Binding
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 76574 0 None -338 4 Human 7.6 pKi = 7.6 Binding
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 76574 0 None -338 4 Human 7.6 pKi = 7.6 Binding
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 76574 0 None -338 4 Human 7.6 pKi = 7.6 Binding
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 91022 0 None -45 3 Human 6.6 pKi = 6.6 Binding
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 91022 0 None -45 3 Human 6.6 pKi = 6.6 Binding
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 91022 0 None -45 3 Human 6.6 pKi = 6.6 Binding
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 91022 0 None -45 3 Human 6.6 pKi = 6.6 Binding
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 68820 0 None 1 2 Human 6.6 pKi = 6.6 Binding
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 68820 0 None 1 2 Human 6.6 pKi = 6.6 Binding
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 166498 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-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 166498 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88873 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88873 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89309 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89309 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89469 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89469 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89470 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89470 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89590 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 89590 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 147612 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 147612 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 190312 0 None -2 4 Human 6.6 pKi = 6.6 Binding
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 190312 0 None -2 4 Human 6.6 pKi = 6.6 Binding
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 190328 0 None -7 3 Human 7.6 pKi = 7.6 Binding
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 190328 0 None -7 3 Human 7.6 pKi = 7.6 Binding
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 106234 0 None -4 2 Human 6.6 pKi = 6.6 Binding
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 106234 0 None -4 2 Human 6.6 pKi = 6.6 Binding
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 105617 0 None -7 3 Human 6.6 pKi = 6.6 Binding
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 105617 0 None -7 3 Human 6.6 pKi = 6.6 Binding
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 65872 0 None -478 4 Human 5.6 pKi = 5.6 Binding
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 65872 0 None -478 4 Human 5.6 pKi = 5.6 Binding
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 66353 0 None -134 3 Human 5.6 pKi = 5.6 Binding
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 66353 0 None -134 3 Human 5.6 pKi = 5.6 Binding
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 88164 0 None -758 3 Human 5.6 pKi = 5.6 Binding
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 88164 0 None -758 3 Human 5.6 pKi = 5.6 Binding
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 10089 0 None -4 4 Human 4.6 pKi = 4.6 Binding
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 10089 0 None -4 4 Human 4.6 pKi = 4.6 Binding
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 88088 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88088 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88743 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 88743 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-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 191116 0 None -4 4 Human 6.6 pKi = 6.6 Binding
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 191116 0 None -4 4 Human 6.6 pKi = 6.6 Binding
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 156555 0 None -218 3 Human 4.6 pKi = 4.6 Binding
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 156555 0 None -218 3 Human 4.6 pKi = 4.6 Binding
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 172779 0 None -56 3 Human 6.6 pKi = 6.6 Binding
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 172779 0 None -56 3 Human 6.6 pKi = 6.6 Binding
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 189398 0 None -28 3 Human 5.6 pKi = 5.6 Binding
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 189398 0 None -28 3 Human 5.6 pKi = 5.6 Binding
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 212348 2 None -41 3 Human 5.5 pKi = 5.5 Binding
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 138984 0 None -5 3 Human 5.5 pKi = 5.5 Binding
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 138984 0 None -5 3 Human 5.5 pKi = 5.5 Binding
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 79584 0 None -3 3 Human 6.5 pKi = 6.5 Binding
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 79584 0 None -3 3 Human 6.5 pKi = 6.5 Binding
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 167876 0 None -112 3 Human 7.5 pKi = 7.5 Binding
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 167876 0 None -112 3 Human 7.5 pKi = 7.5 Binding
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 209024 0 None -33 3 Human 7.5 pKi = 7.5 Binding
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 113936 0 None -6 3 Human 5.5 pKi = 5.5 Binding
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 113936 0 None -6 3 Human 5.5 pKi = 5.5 Binding
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 88169 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88169 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89079 0 None -18 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89079 0 None -18 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 147616 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 147616 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 137849 0 None -18 3 Human 4.5 pKi = 4.5 Binding
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 137849 0 None -18 3 Human 4.5 pKi = 4.5 Binding
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 206717 0 None -52 3 Mouse 6.5 pKi = 6.5 Binding
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 190521 0 None -30 3 Human 6.5 pKi = 6.5 Binding
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 190521 0 None -30 3 Human 6.5 pKi = 6.5 Binding
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 15435 4 None -309 8 Human 5.5 pKi = 5.5 Binding
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 15435 4 None -309 8 Human 5.5 pKi = 5.5 Binding
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 211450 0 None -21 4 Human 8.5 pKi = 8.5 Binding
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 181085 0 None -4 2 Human 8.5 pKi = 8.5 Binding
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 181085 0 None -4 2 Human 8.5 pKi = 8.5 Binding
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 181085 0 None -4 2 Human 8.5 pKi = 8.5 Binding
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 181085 0 None -4 2 Human 8.5 pKi = 8.5 Binding
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 80779 0 None -3 3 Human 8.5 pKi = 8.5 Binding
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 80779 0 None -3 3 Human 8.5 pKi = 8.5 Binding
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 181129 0 None -89 2 Human 8.4 pKi = 8.4 Binding
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 181129 0 None -89 2 Human 8.4 pKi = 8.4 Binding
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 181129 0 None -89 2 Human 8.4 pKi = 8.4 Binding
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 181129 0 None -89 2 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 2649 49 None -72 3 Human 8.4 pKi = 8.4 Binding
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 190007 0 None -4 4 Human 7.5 pKi = 7.5 Binding
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 190007 0 None -4 4 Human 7.5 pKi = 7.5 Binding
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 189894 0 None -10 3 Human 7.5 pKi = 7.5 Binding
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 189894 0 None -10 3 Human 7.5 pKi = 7.5 Binding
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 113937 0 None -5 3 Human 5.5 pKi = 5.5 Binding
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 113937 0 None -5 3 Human 5.5 pKi = 5.5 Binding
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 114562 0 None -52 3 Human 5.5 pKi = 5.5 Binding
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 114562 0 None -52 3 Human 5.5 pKi = 5.5 Binding
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 88136 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88136 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88869 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88869 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89183 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89183 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 212934 0 None -75 3 Human 6.5 pKi = 6.5 Binding
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 172042 0 None -77 3 Human 6.5 pKi = 6.5 Binding
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 172042 0 None -77 3 Human 6.5 pKi = 6.5 Binding
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 182619 0 None -57 2 Human 7.5 pKi = 7.5 Binding
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 182619 0 None -57 2 Human 7.5 pKi = 7.5 Binding
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 182619 0 None -57 2 Human 7.5 pKi = 7.5 Binding
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 182619 0 None -57 2 Human 7.5 pKi = 7.5 Binding
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 173676 0 None -331 3 Human 5.5 pKi = 5.5 Binding
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 173676 0 None -331 3 Human 5.5 pKi = 5.5 Binding
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 173688 0 None -323 3 Human 5.5 pKi = 5.5 Binding
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 173688 0 None -323 3 Human 5.5 pKi = 5.5 Binding
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 188676 0 None -954 3 Human 5.5 pKi = 5.5 Binding
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 188676 0 None -954 3 Human 5.5 pKi = 5.5 Binding
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 88876 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89166 0 None -14 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89166 0 None -14 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89603 0 None -17 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89603 0 None -17 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 96934 0 None -1 4 Human 4.5 pKi = 4.5 Binding
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 96934 0 None -1 4 Human 4.5 pKi = 4.5 Binding
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 211250 0 None -125 3 Human 6.5 pKi = 6.5 Binding
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 203802 73 None -75 34 Human 4.5 pKi = 4.5 Binding
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 203802 73 None -75 34 Human 4.5 pKi = 4.5 Binding
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 203802 73 None -75 34 Human 4.5 pKi = 4.5 Binding
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 212745 0 None -56 3 Human 5.5 pKi = 5.5 Binding
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 204403 0 None -19 4 Human 4.5 pKi = 4.5 Binding
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 204403 0 None -19 4 Human 4.5 pKi = 4.5 Binding
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 138143 0 None -26 3 Human 5.5 pKi = 5.5 Binding
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 138143 0 None -26 3 Human 5.5 pKi = 5.5 Binding
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 137852 0 None -22 3 Human 6.5 pKi = 6.5 Binding
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 137852 0 None -22 3 Human 6.5 pKi = 6.5 Binding
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 137852 0 None -22 3 Human 6.5 pKi = 6.5 Binding
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 137852 0 None -22 3 Human 6.5 pKi = 6.5 Binding
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 126023 0 None -288 3 Human 5.5 pKi = 5.5 Binding
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 126023 0 None -288 3 Human 5.5 pKi = 5.5 Binding
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 88740 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88740 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 173205 0 None -36 3 Human 6.5 pKi = 6.5 Binding
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 173205 0 None -36 3 Human 6.5 pKi = 6.5 Binding
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 158900 0 None -83 3 Human 6.5 pKi = 6.5 Binding
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 158900 0 None -83 3 Human 6.5 pKi = 6.5 Binding
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 65354 0 None -1 4 Human 7.5 pKi = 7.5 Binding
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 65354 0 None -1 4 Human 7.5 pKi = 7.5 Binding
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 210957 0 None -77 3 Human 7.5 pKi = 7.5 Binding
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 147662 0 None -1318 4 Human 5.5 pKi = 5.5 Binding
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 147662 0 None -1318 4 Human 5.5 pKi = 5.5 Binding
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 88876 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89817 0 None -20 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 89817 0 None -20 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 145284 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 145284 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 145935 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 145935 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-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 204762 0 None -21 4 Human 4.5 pKi = 4.5 Binding
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 204762 0 None -21 4 Human 4.5 pKi = 4.5 Binding
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 187469 0 None -97 7 Rat 6.5 pKi = 6.5 Binding
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 187469 0 None -97 7 Rat 6.5 pKi = 6.5 Binding
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 96565 0 None -100 6 Mouse 6.5 pKi = 6.5 Binding
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 96565 0 None -100 6 Mouse 6.5 pKi = 6.5 Binding
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 208224 0 None -28 3 Human 5.5 pKi = 5.5 Binding
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 139851 0 None -467 4 Human 5.5 pKi = 5.5 Binding
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 139851 0 None -467 4 Human 5.5 pKi = 5.5 Binding
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 141017 0 None -17 3 Human 7.5 pKi = 7.5 Binding
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 141017 0 None -17 3 Human 7.5 pKi = 7.5 Binding
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 191807 0 None -56 3 Human 7.5 pKi = 7.5 Binding
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 191807 0 None -56 3 Human 7.5 pKi = 7.5 Binding
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 204820 0 None -3 3 Human 6.5 pKi = 6.5 Binding
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 204820 0 None -3 3 Human 6.5 pKi = 6.5 Binding
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 66356 0 None -1659 3 Human 5.5 pKi = 5.5 Binding
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 66356 0 None -1659 3 Human 5.5 pKi = 5.5 Binding
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 95274 0 None 1 2 Human 5.5 pKi = 5.5 Binding
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 95274 0 None 1 2 Human 5.5 pKi = 5.5 Binding
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 123137 0 None 1 3 Human 4.5 pKi = 4.5 Binding
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 123137 0 None 1 3 Human 4.5 pKi = 4.5 Binding
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 80906 0 None -58 3 Human 6.5 pKi = 6.5 Binding
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 80906 0 None -58 3 Human 6.5 pKi = 6.5 Binding
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 164719 0 None -33 4 Human 5.4 pKi = 5.4 Binding
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 164719 0 None -33 4 Human 5.4 pKi = 5.4 Binding
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 66002 0 None -281 4 Human 5.4 pKi = 5.4 Binding
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 66002 0 None -281 4 Human 5.4 pKi = 5.4 Binding
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 88741 0 None -17 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 88741 0 None -17 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89471 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89471 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 191190 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 191190 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 191592 0 None -16 3 Human 7.4 pKi = 7.4 Binding
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 191592 0 None -16 3 Human 7.4 pKi = 7.4 Binding
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 106535 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 106535 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 88131 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-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 88131 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-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 10086 0 None -16 4 Human 4.4 pKi = 4.4 Binding
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 10086 0 None -16 4 Human 4.4 pKi = 4.4 Binding
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 89805 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89805 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147863 0 None -15 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147863 0 None -15 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 171428 0 None -34 3 Human 6.4 pKi = 6.4 Binding
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 171428 0 None -34 3 Human 6.4 pKi = 6.4 Binding
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 190684 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 190684 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 106514 0 None -4 3 Human 6.4 pKi = 6.4 Binding
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 106514 0 None -4 3 Human 6.4 pKi = 6.4 Binding
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 187517 0 None -70 4 Human 6.4 pKi = 6.4 Binding
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 187517 0 None -70 4 Human 6.4 pKi = 6.4 Binding
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 213503 0 None -37 3 Human 6.4 pKi = 6.4 Binding
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 88267 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 88267 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89308 0 None -6 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89308 0 None -6 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 168321 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 168321 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 139654 0 None -5 3 Human 6.4 pKi = 6.4 Binding
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 139654 0 None -5 3 Human 6.4 pKi = 6.4 Binding
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 79352 0 None -6 3 Human 5.4 pKi = 5.4 Binding
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 79352 0 None -6 3 Human 5.4 pKi = 5.4 Binding
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 212708 0 None -346 3 Human 6.4 pKi = 6.4 Binding
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 213479 0 None -138 3 Human 6.4 pKi = 6.4 Binding
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 157002 0 None -8 3 Human 4.4 pKi = 4.4 Binding
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 157002 0 None -8 3 Human 4.4 pKi = 4.4 Binding
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 200133 0 None -2 3 Human 6.4 pKi = 6.4 Binding
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 200133 0 None -2 3 Human 6.4 pKi = 6.4 Binding
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 70742 0 None -134 3 Human 6.4 pKi = 6.4 Binding
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 70742 0 None -134 3 Human 6.4 pKi = 6.4 Binding
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 123838 0 None -354 3 Human 5.4 pKi = 5.4 Binding
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 123838 0 None -354 3 Human 5.4 pKi = 5.4 Binding
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 176945 0 None -1 4 Human 5.4 pKi = 5.4 Binding
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 176945 0 None -1 4 Human 5.4 pKi = 5.4 Binding
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 89804 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89804 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147860 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147860 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 158672 0 None -416 3 Human 5.4 pKi = 5.4 Binding
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 158672 0 None -416 3 Human 5.4 pKi = 5.4 Binding
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 191300 0 None -20 3 Human 5.4 pKi = 5.4 Binding
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 191300 0 None -20 3 Human 5.4 pKi = 5.4 Binding
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 213230 0 None -20 3 Human 5.4 pKi = 5.4 Binding
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 210607 0 None -173 3 Human 6.4 pKi = 6.4 Binding
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 210002 1 None -31 3 Mouse 6.4 pKi = 6.4 Binding
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 86839 4 None -204 4 Human 6.4 pKi = 6.4 Binding
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 86839 4 None -204 4 Human 6.4 pKi = 6.4 Binding
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 88744 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 88744 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 79643 0 None -2 3 Human 6.4 pKi = 6.4 Binding
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 79643 0 None -2 3 Human 6.4 pKi = 6.4 Binding
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 212657 0 None -51 3 Human 6.4 pKi = 6.4 Binding
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 190684 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 190684 0 None -2 4 Human 7.4 pKi = 7.4 Binding
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 89803 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89803 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 80099 0 None -21 3 Human 5.4 pKi = 5.4 Binding
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 80099 0 None -21 3 Human 5.4 pKi = 5.4 Binding
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 80099 0 None -21 3 Human 5.4 pKi = 5.4 Binding
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 80099 0 None -21 3 Human 5.4 pKi = 5.4 Binding
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 77710 0 None -6 3 Human 5.4 pKi = 5.4 Binding
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 77710 0 None -6 3 Human 5.4 pKi = 5.4 Binding
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 76572 0 None -245 4 Human 7.4 pKi = 7.4 Binding
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 76572 0 None -245 4 Human 7.4 pKi = 7.4 Binding
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 76572 0 None -245 4 Human 7.4 pKi = 7.4 Binding
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 76572 0 None -245 4 Human 7.4 pKi = 7.4 Binding
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 138119 0 None -1 3 Human 7.4 pKi = 7.4 Binding
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 138119 0 None -1 3 Human 7.4 pKi = 7.4 Binding
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 211895 0 None -104 3 Human 6.4 pKi = 6.4 Binding
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 165948 0 None -177 5 Human 6.4 pKi = 6.4 Binding
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 165948 0 None -177 5 Human 6.4 pKi = 6.4 Binding
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 139642 0 None -398 4 Human 5.4 pKi = 5.4 Binding
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 139642 0 None -398 4 Human 5.4 pKi = 5.4 Binding
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 158945 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 158945 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 139549 0 None -3 3 Human 6.4 pKi = 6.4 Binding
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 139549 0 None -3 3 Human 6.4 pKi = 6.4 Binding
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 158061 0 None -18 3 Human 4.4 pKi = 4.4 Binding
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 158061 0 None -18 3 Human 4.4 pKi = 4.4 Binding
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 173012 0 None -11 3 Human 6.4 pKi = 6.4 Binding
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 173012 0 None -11 3 Human 6.4 pKi = 6.4 Binding
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 211996 0 None 1 3 Human 7.4 pKi = 7.4 Binding
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 89599 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-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 146066 0 None -12 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 146066 0 None -12 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147416 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 147416 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 172374 0 None -16 3 Human 6.4 pKi = 6.4 Binding
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 172374 0 None -16 3 Human 6.4 pKi = 6.4 Binding
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 137098 0 None -10 3 Human 5.4 pKi = 5.4 Binding
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 137098 0 None -10 3 Human 5.4 pKi = 5.4 Binding
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 204804 0 None -12 3 Human 6.4 pKi = 6.4 Binding
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 204804 0 None -12 3 Human 6.4 pKi = 6.4 Binding
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 214128 0 None -6 3 Human 6.4 pKi = 6.4 Binding
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 125821 0 None -269 4 Human 5.4 pKi = 5.4 Binding
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 125821 0 None -269 4 Human 5.4 pKi = 5.4 Binding
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 89479 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89479 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 151009 0 None -4 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 151009 0 None -4 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 207439 0 None -9 4 Human 7.4 pKi = 7.4 Binding
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 123542 0 None -316 2 Human 6.4 pKi = 6.4 Binding
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 123542 0 None -316 2 Human 6.4 pKi = 6.4 Binding
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 207442 0 None -57 4 Human 6.4 pKi = 6.4 Binding
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 88270 0 None -562 3 Human 6.4 pKi = 6.4 Binding
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 88270 0 None -562 3 Human 6.4 pKi = 6.4 Binding
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 178071 0 None -134 4 Human 6.4 pKi = 6.4 Binding
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 178071 0 None -134 4 Human 6.4 pKi = 6.4 Binding
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 3747 37 None -70 4 Human 5.4 pKi = 5.4 Binding
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 3747 37 None -70 4 Human 5.4 pKi = 5.4 Binding
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 3747 37 None -70 4 Human 5.4 pKi = 5.4 Binding
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 87025 0 None -1148 3 Human 5.4 pKi = 5.4 Binding
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 87025 0 None -1148 3 Human 5.4 pKi = 5.4 Binding
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 154885 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 154885 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 88322 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 88322 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89475 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 89475 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 146323 0 None -23 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 146323 0 None -23 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 151052 0 None -2 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 151052 0 None -2 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-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 204632 0 None -3 3 Human 4.4 pKi = 4.4 Binding
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 204632 0 None -3 3 Human 4.4 pKi = 4.4 Binding
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 57918 0 None -13 4 Human 5.3 pKi = 5.3 Binding
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 57918 0 None -13 4 Human 5.3 pKi = 5.3 Binding
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 207534 31 None -30 4 Human 7.3 pKi = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pKi = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pKi = 7.3 Binding
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 207534 31 None -30 4 Human 7.3 pKi = 7.3 Binding
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 139855 0 None -263 4 Human 5.3 pKi = 5.3 Binding
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 139855 0 None -263 4 Human 5.3 pKi = 5.3 Binding
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 146067 0 None -15 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 146067 0 None -15 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 170458 0 None -16 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 170458 0 None -16 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 79718 0 None -1 3 Human 6.3 pKi = 6.3 Binding
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 79718 0 None -1 3 Human 6.3 pKi = 6.3 Binding
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 76172 0 None -36 3 Human 6.3 pKi = 6.3 Binding
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 76172 0 None -36 3 Human 6.3 pKi = 6.3 Binding
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 16457 0 None -53 3 Human 7.3 pKi = 7.3 Binding
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 16457 0 None -53 3 Human 7.3 pKi = 7.3 Binding
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 79774 0 None -42 3 Human 6.3 pKi = 6.3 Binding
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 79774 0 None -42 3 Human 6.3 pKi = 6.3 Binding
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 79774 0 None -42 3 Human 6.3 pKi = 6.3 Binding
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 79774 0 None -42 3 Human 6.3 pKi = 6.3 Binding
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 88087 0 None -23 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88087 0 None -23 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88982 0 None -5 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88982 0 None -5 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 172127 0 None -33 3 Human 6.3 pKi = 6.3 Binding
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 172127 0 None -33 3 Human 6.3 pKi = 6.3 Binding
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 213525 0 None -602 3 Human 6.3 pKi = 6.3 Binding
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 212148 0 None 1 2 Human 6.3 pKi = 6.3 Binding
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 105618 0 None -1 3 Human 5.3 pKi = 5.3 Binding
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 105618 0 None -1 3 Human 5.3 pKi = 5.3 Binding
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 88186 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88186 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 68315 0 None 1 2 Human 5.3 pKi = 5.3 Binding
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 68315 0 None 1 2 Human 5.3 pKi = 5.3 Binding
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 187469 0 None -141 7 Human 6.3 pKi = 6.3 Binding
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 187469 0 None -141 7 Human 6.3 pKi = 6.3 Binding
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 151371 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 151371 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 190363 0 None -89 3 Human 8.3 pKi = 8.3 Binding
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 190363 0 None -89 3 Human 8.3 pKi = 8.3 Binding
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 190352 0 None -14 3 Human 8.3 pKi = 8.3 Binding
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 190352 0 None -14 3 Human 8.3 pKi = 8.3 Binding
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 211026 0 None 1 3 Human 8.3 pKi = 8.3 Binding
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 105528 0 None 4 3 Human 8.2 pKi = 8.2 Binding
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 105528 0 None 4 3 Human 8.2 pKi = 8.2 Binding
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 208764 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 77661 0 None -2 3 Human 7.3 pKi = 7.3 Binding
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 77661 0 None -2 3 Human 7.3 pKi = 7.3 Binding
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 213346 0 None -69 3 Human 7.3 pKi = 7.3 Binding
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 78618 0 None 7 4 Human 6.3 pKi = 6.3 Binding
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 78618 0 None 7 4 Human 6.3 pKi = 6.3 Binding
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 138229 0 None -741 3 Human 5.3 pKi = 5.3 Binding
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 138229 0 None -741 3 Human 5.3 pKi = 5.3 Binding
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 88225 0 None -4 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88225 0 None -4 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88871 0 None -33 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88871 0 None -33 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 89816 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 89816 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 137068 0 None 1 3 Human 6.3 pKi = 6.3 Binding
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 137068 0 None 1 3 Human 6.3 pKi = 6.3 Binding
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 105618 0 None -1 3 Human 5.3 pKi = 5.3 Binding
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 105618 0 None -1 3 Human 5.3 pKi = 5.3 Binding
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 213526 0 None -120 3 Human 5.3 pKi = 5.3 Binding
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 96942 0 None -79 4 Human 4.3 pKi = 4.3 Binding
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 96942 0 None -79 4 Human 4.3 pKi = 4.3 Binding
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 189914 0 None -23 3 Human 7.3 pKi = 7.3 Binding
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 189914 0 None -23 3 Human 7.3 pKi = 7.3 Binding
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 213349 0 None -741 3 Human 7.3 pKi = 7.3 Binding
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 89349 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 89349 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 89805 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 89805 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 96143 0 None -13 4 Human 5.3 pKi = 5.3 Binding
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 96143 0 None -13 4 Human 5.3 pKi = 5.3 Binding
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 88133 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88133 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 153892 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 153892 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 78706 0 None -4 4 Human 4.3 pKi = 4.3 Binding
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 78706 0 None -4 4 Human 4.3 pKi = 4.3 Binding
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 133094 0 None -2 2 Human 6.3 pKi = 6.3 Binding
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 133094 0 None -2 2 Human 6.3 pKi = 6.3 Binding
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 138763 0 None -5 3 Human 6.3 pKi = 6.3 Binding
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 138763 0 None -5 3 Human 6.3 pKi = 6.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 205261 0 None -3 4 Human 4.3 pKi = 4.3 Binding
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 205261 0 None -3 4 Human 4.3 pKi = 4.3 Binding
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 88224 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 88224 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 158775 0 None -102 3 Human 4.3 pKi = 4.3 Binding
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 158775 0 None -102 3 Human 4.3 pKi = 4.3 Binding
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 161375 0 None -17 3 Human 7.3 pKi = 7.3 Binding
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 161375 0 None -17 3 Human 7.3 pKi = 7.3 Binding
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 161375 0 None -17 3 Human 7.3 pKi = 7.3 Binding
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 156841 0 None -11 3 Human 6.3 pKi = 6.3 Binding
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 156841 0 None -11 3 Human 6.3 pKi = 6.3 Binding
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 204489 0 None -8 3 Human 6.3 pKi = 6.3 Binding
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 204489 0 None -8 3 Human 6.3 pKi = 6.3 Binding
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 145768 0 None -562 4 Human 6.3 pKi = 6.3 Binding
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 145768 0 None -562 4 Human 6.3 pKi = 6.3 Binding
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 145279 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 145279 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 145282 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 145282 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 148260 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 148260 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-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 208872 0 None -70 3 Human 7.3 pKi = 7.3 Binding
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 148666 0 None -54 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 148666 0 None -54 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-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 74647 0 None -1479 3 Human 4.3 pKi = 4.3 Binding
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 74647 0 None -1479 3 Human 4.3 pKi = 4.3 Binding
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 113924 0 None -151 3 Human 7.3 pKi = 7.3 Binding
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 113924 0 None -151 3 Human 7.3 pKi = 7.3 Binding
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 209488 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
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 208992 0 None -102 3 Human 7.3 pKi = 7.3 Binding
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 70269 0 None -281 4 Human 6.3 pKi = 6.3 Binding
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 70269 0 None -281 4 Human 6.3 pKi = 6.3 Binding
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 155159 0 None -5 4 Human 5.3 pKi = 5.3 Binding
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 155159 0 None -5 4 Human 5.3 pKi = 5.3 Binding
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 205492 0 None -6 3 Human 4.3 pKi = 4.3 Binding
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 205492 0 None -6 3 Human 4.3 pKi = 4.3 Binding
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 96942 0 None -79 4 Human 4.3 pKi = 4.3 Binding
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 96942 0 None -79 4 Human 4.3 pKi = 4.3 Binding
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 70386 0 None -239 3 Human 6.2 pKi = 6.2 Binding
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 70386 0 None -239 3 Human 6.2 pKi = 6.2 Binding
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 178090 0 None -57 3 Human 6.2 pKi = 6.2 Binding
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 178090 0 None -57 3 Human 6.2 pKi = 6.2 Binding
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 89386 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 89386 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 88095 0 None -26 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 88095 0 None -26 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89808 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89808 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 203949 1 None -1 3 Human 4.2 pKi = 4.2 Binding
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 203949 1 None -1 3 Human 4.2 pKi = 4.2 Binding
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 70277 0 None -446 2 Human 6.2 pKi = 6.2 Binding
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 70277 0 None -446 2 Human 6.2 pKi = 6.2 Binding
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 96284 0 None -15 3 Human 6.2 pKi = 6.2 Binding
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 96284 0 None -15 3 Human 6.2 pKi = 6.2 Binding
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 147382 0 None -7 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 147382 0 None -7 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 96519 0 None -2 4 Human 4.2 pKi = 4.2 Binding
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 96519 0 None -2 4 Human 4.2 pKi = 4.2 Binding
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 165948 0 None -177 5 Human 6.2 pKi = 6.2 Binding
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 165948 0 None -177 5 Human 6.2 pKi = 6.2 Binding
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 113610 0 None -6 3 Human 5.2 pKi = 5.2 Binding
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 113610 0 None -6 3 Human 5.2 pKi = 5.2 Binding
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 163356 0 None -1 3 Human 5.2 pKi = 5.2 Binding
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 163356 0 None -1 3 Human 5.2 pKi = 5.2 Binding
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 167500 0 None -1 3 Human 5.2 pKi = 5.2 Binding
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 167500 0 None -1 3 Human 5.2 pKi = 5.2 Binding
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 168062 0 None -4 3 Human 5.2 pKi = 5.2 Binding
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 168062 0 None -4 3 Human 5.2 pKi = 5.2 Binding
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 89818 0 None -21 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89818 0 None -21 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 203753 13 None -4 3 Human 4.2 pKi = 4.2 Binding
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 203753 13 None -4 3 Human 4.2 pKi = 4.2 Binding
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 212077 0 None -2 3 Human 8.2 pKi = 8.2 Binding
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 211253 0 None -22 4 Human 8.2 pKi = 8.2 Binding
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 147625 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 147625 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 79605 0 None -16 3 Human 5.2 pKi = 5.2 Binding
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 79605 0 None -16 3 Human 5.2 pKi = 5.2 Binding
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 168179 0 None -1230 3 Human 5.2 pKi = 5.2 Binding
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 168179 0 None -1230 3 Human 5.2 pKi = 5.2 Binding
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 89313 0 None -27 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89313 0 None -27 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 96756 0 None -5 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 96756 0 None -5 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 65748 0 None -131 3 Human 6.2 pKi = 6.2 Binding
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 65748 0 None -131 3 Human 6.2 pKi = 6.2 Binding
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 106628 0 None -5 3 Human 6.2 pKi = 6.2 Binding
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 106628 0 None -5 3 Human 6.2 pKi = 6.2 Binding
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 209998 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
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 209999 0 None -10 2 Mouse 6.2 pKi = 6.2 Binding
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 210003 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
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 89084 0 None -5 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89084 0 None -5 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89303 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89303 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148982 0 None -9 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148982 0 None -9 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 190116 0 None -109 3 Human 5.2 pKi = 5.2 Binding
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 190116 0 None -109 3 Human 5.2 pKi = 5.2 Binding
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 126536 1 None -134 4 Human 6.2 pKi = 6.2 Binding
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 126536 1 None -134 4 Human 6.2 pKi = 6.2 Binding
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 88921 0 None -144 3 Human 6.2 pKi = 6.2 Binding
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 88921 0 None -144 3 Human 6.2 pKi = 6.2 Binding
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 126536 1 None -134 4 Human 6.2 pKi = 6.2 Binding
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 126536 1 None -134 4 Human 6.2 pKi = 6.2 Binding
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 10084 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 10084 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 89598 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 89598 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 167515 0 None -10 3 Human 7.2 pKi = 7.2 Binding
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 167515 0 None -10 3 Human 7.2 pKi = 7.2 Binding
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 123513 0 None -85 4 Human 6.2 pKi = 6.2 Binding
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 123513 0 None -85 4 Human 6.2 pKi = 6.2 Binding
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 123349 0 None -7 4 Human 5.2 pKi = 5.2 Binding
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 123349 0 None -7 4 Human 5.2 pKi = 5.2 Binding
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 88092 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 88092 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148070 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148070 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148258 0 None -30 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 148258 0 None -30 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 166039 0 None -11 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 166039 0 None -11 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 161170 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 161170 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 204878 0 None -3 3 Human 7.2 pKi = 7.2 Binding
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 204878 0 None -3 3 Human 7.2 pKi = 7.2 Binding
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 89599 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 89599 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 76570 0 None -338 4 Human 7.2 pKi = 7.2 Binding
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 76570 0 None -338 4 Human 7.2 pKi = 7.2 Binding
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 76570 0 None -338 4 Human 7.2 pKi = 7.2 Binding
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 76570 0 None -338 4 Human 7.2 pKi = 7.2 Binding
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 70518 0 None -446 4 Human 6.2 pKi = 6.2 Binding
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 70518 0 None -446 4 Human 6.2 pKi = 6.2 Binding
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 145776 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 145776 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 211057 0 None -3 3 Human 7.2 pKi = 7.2 Binding
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 122587 0 None -4 4 Human 5.2 pKi = 5.2 Binding
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 122587 0 None -4 4 Human 5.2 pKi = 5.2 Binding
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 77466 0 None -7 3 Human 4.2 pKi = 4.2 Binding
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 77466 0 None -7 3 Human 4.2 pKi = 4.2 Binding
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 88581 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 88581 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-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 190541 0 None -2 4 Human 7.2 pKi = 7.2 Binding
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 190541 0 None -2 4 Human 7.2 pKi = 7.2 Binding
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 1473 6 None 1 3 Human 6.2 pKi = 6.2 Binding
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 1473 6 None 1 3 Human 6.2 pKi = 6.2 Binding
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 1473 6 None 1 3 Human 6.2 pKi = 6.2 Binding
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 68288 0 None -2 2 Human 6.2 pKi = 6.2 Binding
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 68288 0 None -2 2 Human 6.2 pKi = 6.2 Binding
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 140914 0 None -5 3 Human 8.2 pKi = 8.2 Binding
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 140914 0 None -5 3 Human 8.2 pKi = 8.2 Binding
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 168430 0 None 7 3 Human 8.1 pKi = 8.1 Binding
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 168430 0 None 7 3 Human 8.1 pKi = 8.1 Binding
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 208634 0 None -15 3 Human 8.1 pKi = 8.1 Binding
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 119469 0 None -114 3 Human 5.2 pKi = 5.2 Binding
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 119469 0 None -114 3 Human 5.2 pKi = 5.2 Binding
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 138180 1 None -239 4 Human 5.2 pKi = 5.2 Binding
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 138180 1 None -239 4 Human 5.2 pKi = 5.2 Binding
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 77592 0 None -46 3 Human 6.2 pKi = 6.2 Binding
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 77592 0 None -46 3 Human 6.2 pKi = 6.2 Binding
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 10204 0 None 1 2 Human 5.2 pKi = 5.2 Binding
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 10204 0 None 1 2 Human 5.2 pKi = 5.2 Binding
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 213705 0 None -60 3 Human 6.2 pKi = 6.2 Binding
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 207443 0 None -123 4 Human 7.2 pKi = 7.2 Binding
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 91169 0 None -123 3 Human 6.2 pKi = 6.2 Binding
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 91169 0 None -123 3 Human 6.2 pKi = 6.2 Binding
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 91169 0 None -123 3 Human 6.2 pKi = 6.2 Binding
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 91169 0 None -123 3 Human 6.2 pKi = 6.2 Binding
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 96565 0 None -208 6 Human 6.2 pKi = 6.2 Binding
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 96565 0 None -208 6 Human 6.2 pKi = 6.2 Binding
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 66432 0 None -93 3 Human 6.2 pKi = 6.2 Binding
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 66432 0 None -93 3 Human 6.2 pKi = 6.2 Binding
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 88876 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 88876 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-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 77711 0 None -4 3 Human 5.1 pKi = 5.1 Binding
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 77711 0 None -4 3 Human 5.1 pKi = 5.1 Binding
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 79148 0 None -1548 3 Human 5.1 pKi = 5.1 Binding
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 79148 0 None -1548 3 Human 5.1 pKi = 5.1 Binding
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 176150 0 None -9 3 Human 6.1 pKi = 6.1 Binding
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 176150 0 None -9 3 Human 6.1 pKi = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pKi = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pKi = 6.1 Binding
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 3747 37 None -70 4 Human 6.1 pKi = 6.1 Binding
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 89484 0 None -7 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 89484 0 None -7 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 79820 0 None -21 3 Human 5.1 pKi = 5.1 Binding
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 79820 0 None -21 3 Human 5.1 pKi = 5.1 Binding
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 138696 0 None -10 3 Human 7.1 pKi = 7.1 Binding
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 138696 0 None -10 3 Human 7.1 pKi = 7.1 Binding
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 147650 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
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 147650 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
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 147650 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
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 147650 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
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 89597 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 89597 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 157419 0 None -1318 3 Human 5.1 pKi = 5.1 Binding
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 157419 0 None -1318 3 Human 5.1 pKi = 5.1 Binding
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 168941 0 None -53 3 Human 7.1 pKi = 7.1 Binding
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 168941 0 None -53 3 Human 7.1 pKi = 7.1 Binding
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 153883 0 None -1258 4 Human 6.1 pKi = 6.1 Binding
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 153883 0 None -1258 4 Human 6.1 pKi = 6.1 Binding
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 205199 0 None -13 3 Human 7.1 pKi = 7.1 Binding
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 205199 0 None -13 3 Human 7.1 pKi = 7.1 Binding
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 212348 2 None -41 3 Human 6.1 pKi = 6.1 Binding
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 10202 0 None 4 2 Human 5.1 pKi = 5.1 Binding
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 10202 0 None 4 2 Human 5.1 pKi = 5.1 Binding
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 148981 0 None -26 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 148981 0 None -26 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 153858 0 None -16 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 153858 0 None -16 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 123806 0 None -467 3 Human 6.1 pKi = 6.1 Binding
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 123806 0 None -467 3 Human 6.1 pKi = 6.1 Binding
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 168057 1 None -245 4 Human 6.1 pKi = 6.1 Binding
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 168057 1 None -245 4 Human 6.1 pKi = 6.1 Binding
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 120739 0 None -50 2 Mouse 6.1 pKi = 6.1 Binding
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 120739 0 None -50 2 Mouse 6.1 pKi = 6.1 Binding
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 209997 0 None -2 2 Mouse 6.1 pKi = 6.1 Binding
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 96602 0 None -13 4 Human 5.1 pKi = 5.1 Binding
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 96602 0 None -13 4 Human 5.1 pKi = 5.1 Binding
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 76571 0 None -23 4 Human 8.1 pKi = 8.1 Binding
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 76571 0 None -23 4 Human 8.1 pKi = 8.1 Binding
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 76569 0 None -74 4 Human 8.1 pKi = 8.1 Binding
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 76569 0 None -74 4 Human 8.1 pKi = 8.1 Binding
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 76569 0 None -74 4 Human 8.1 pKi = 8.1 Binding
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 76569 0 None -74 4 Human 8.1 pKi = 8.1 Binding
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 181983 0 None -6 2 Human 8.1 pKi = 8.1 Binding
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 181983 0 None -6 2 Human 8.1 pKi = 8.1 Binding
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 181983 0 None -6 2 Human 8.1 pKi = 8.1 Binding
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 181983 0 None -6 2 Human 8.1 pKi = 8.1 Binding
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 171200 0 None -14 3 Human 7.1 pKi = 7.1 Binding
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 171200 0 None -14 3 Human 7.1 pKi = 7.1 Binding
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 69960 0 None -173 2 Human 6.1 pKi = 6.1 Binding
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 69960 0 None -173 2 Human 6.1 pKi = 6.1 Binding
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 80710 0 None -61 3 Human 6.1 pKi = 6.1 Binding
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 80710 0 None -61 3 Human 6.1 pKi = 6.1 Binding
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 89345 0 None -21 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 89345 0 None -21 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-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 135365 0 None -162 2 Human 6.1 pKi = 6.1 Binding
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 135365 0 None -162 2 Human 6.1 pKi = 6.1 Binding
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 148259 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 148259 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 79819 0 None -426 3 Human 5.1 pKi = 5.1 Binding
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 79819 0 None -426 3 Human 5.1 pKi = 5.1 Binding
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 88657 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
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 88657 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
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 88657 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
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 88657 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
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 78634 0 None -117 4 Human 5.1 pKi = 5.1 Binding
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 78634 0 None -117 4 Human 5.1 pKi = 5.1 Binding
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 10088 0 None -28 2 Human 4.1 pKi = 4.1 Binding
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 10088 0 None -28 2 Human 4.1 pKi = 4.1 Binding
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 138373 0 None -64 3 Human 6.1 pKi = 6.1 Binding
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 138373 0 None -64 3 Human 6.1 pKi = 6.1 Binding
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 188336 0 None -43 3 Human 6.1 pKi = 6.1 Binding
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 188336 0 None -43 3 Human 6.1 pKi = 6.1 Binding
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 190541 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 190541 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 68330 0 None -295 2 Human 6.1 pKi = 6.1 Binding
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 68330 0 None -295 2 Human 6.1 pKi = 6.1 Binding
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 150811 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 150811 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-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 191074 0 None -169 3 Human 5.1 pKi = 5.1 Binding
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 191074 0 None -169 3 Human 5.1 pKi = 5.1 Binding
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 77596 0 None -8 3 Human 6.1 pKi = 6.1 Binding
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 77596 0 None -8 3 Human 6.1 pKi = 6.1 Binding
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 213097 0 None -93 3 Human 7.1 pKi = 7.1 Binding
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 79948 0 None -8 3 Human 7.1 pKi = 7.1 Binding
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 79948 0 None -8 3 Human 7.1 pKi = 7.1 Binding
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 68060 0 None -407 2 Human 6.1 pKi = 6.1 Binding
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 68060 0 None -407 2 Human 6.1 pKi = 6.1 Binding
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 96928 9 None -4 3 Human 4.1 pKi = 4.1 Binding
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 96928 9 None -4 3 Human 4.1 pKi = 4.1 Binding
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 69482 0 None -18 2 Human 6.1 pKi = 6.1 Binding
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 69482 0 None -18 2 Human 6.1 pKi = 6.1 Binding
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 169991 0 None -15 3 Human 5.1 pKi = 5.1 Binding
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 169991 0 None -15 3 Human 5.1 pKi = 5.1 Binding
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 63941 0 None -16 4 Human 5.1 pKi = 5.1 Binding
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 63941 0 None -16 4 Human 5.1 pKi = 5.1 Binding
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 116449 0 None -39 4 Human 5.1 pKi = 5.1 Binding
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 116449 0 None -39 4 Human 5.1 pKi = 5.1 Binding
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 191713 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 191713 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 214122 0 None -17 3 Human 6.1 pKi = 6.1 Binding
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 212714 0 None -575 3 Human 6.1 pKi = 6.1 Binding
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 213613 0 None -1258 3 Human 6.1 pKi = 6.1 Binding
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 211690 0 None -17 4 Human 8.0 pKi = 8.0 Binding
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 191713 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 191713 0 None -2 4 Human 7.1 pKi = 7.1 Binding
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 135152 0 None -3 2 Human 6.1 pKi = 6.1 Binding
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 135152 0 None -3 2 Human 6.1 pKi = 6.1 Binding
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 96602 0 None -13 4 Human 5.1 pKi = 5.1 Binding
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 96602 0 None -13 4 Human 5.1 pKi = 5.1 Binding
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 88229 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 88229 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 94990 0 None -1 2 Human 5.0 pKi = 5.0 Binding
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 94990 0 None -1 2 Human 5.0 pKi = 5.0 Binding
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 189669 0 None -83 3 Human 5.0 pKi = 5.0 Binding
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 189669 0 None -83 3 Human 5.0 pKi = 5.0 Binding
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 166947 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 166947 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 89474 0 None -15 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 89474 0 None -15 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 88266 0 None -100 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-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 88266 0 None -100 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-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 176184 0 None -5 3 Human 6.0 pKi = 6.0 Binding
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 176184 0 None -5 3 Human 6.0 pKi = 6.0 Binding
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 124648 0 None -478 2 Human 6.0 pKi = 6.0 Binding
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 124648 0 None -478 2 Human 6.0 pKi = 6.0 Binding
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 88746 0 None -213 3 Human 6.0 pKi = 6.0 Binding
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 88746 0 None -213 3 Human 6.0 pKi = 6.0 Binding
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 88272 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 88272 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-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 190807 0 None -3 4 Human 7.0 pKi = 7.0 Binding
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 190807 0 None -3 4 Human 7.0 pKi = 7.0 Binding
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 211251 0 None -79 3 Human 7.0 pKi = 7.0 Binding
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 189793 0 None -87 3 Human 5.0 pKi = 5.0 Binding
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 189793 0 None -87 3 Human 5.0 pKi = 5.0 Binding
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 166698 0 None -9 3 Human 4.0 pKi = 4 Binding
Displacement of [125I]NDP-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 166698 0 None -9 3 Human 4.0 pKi = 4 Binding
Displacement of [125I]NDP-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 427 0 None - 1 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
70669253 427 0 None - 1 Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
1321 1911 0 None -15 3 Human 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
1328 1912 0 None -15 4 Human 8.3 pKd None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9832440
1333 1733 0 None - 1 Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
44134812 1733 0 None - 1 Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
None 214558 0 125I-NDP-MSH -11 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
None 214558 0 125I-[Nle4,D-Phe7]Alpha-MSH -11 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 299 5 3 6 -0.3 CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O None
3198 203802 73 None -75 34 Human 8.4 pKi = 8.4 Binding
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 203802 73 None -75 34 Human 8.4 pKi = 8.4 Binding
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 203802 73 None -75 34 Human 8.4 pKi = 8.4 Binding
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 906 64 None -186 72 Human 8.3 pKi = 8.3 Binding
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
621 906 64 None -186 72 Human 8.3 pKi = 8.3 Binding
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
83 906 64 None -186 72 Human 8.3 pKi = 8.3 Binding
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 906 64 None -186 72 Human 8.3 pKi = 8.3 Binding
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 906 64 None -186 72 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 3690 75 None -56 35 Human 8.3 pKi = 8.3 Binding
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 205195 91 None -54 34 Human 8.3 pKi = 8.3 Binding
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 205195 91 None -54 34 Human 8.3 pKi = 8.3 Binding
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 205195 91 None -54 34 Human 8.3 pKi = 8.3 Binding
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 502 77 None -147 41 Human 8.3 pKi = 8.3 Binding
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
249 502 77 None -147 41 Human 8.3 pKi = 8.3 Binding
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 502 77 None -147 41 Human 8.3 pKi = 8.3 Binding
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 502 77 None -147 41 Human 8.3 pKi = 8.3 Binding
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 502 77 None -147 41 Human 8.3 pKi = 8.3 Binding
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
176 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
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 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
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 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
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 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
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 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
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 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
16132265 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
3633 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
4931 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201610 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
DB01285 274 0 None -5 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central None None None None None
None 214559 0 125I-NDP-MSH -7 4 Human 6.1 pKi = 6.1 Binding
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 214559 0 125I-[Nle4,D-Phe7]Alpha-MSH -7 4 Human 6.1 pKi = 6.1 Binding
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 3536 18 None -3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
5416 3536 18 None -3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
9272 3536 18 None -3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL3301624 3536 18 None -3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB11700 3536 18 None -3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
131839615 210889 20 None -1 2 Human 8.1 pKi = 8.1 Binding
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 210889 20 None -1 2 Human 8.1 pKi = 8.1 Binding
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 210889 20 None -1 2 Human 8.1 pKi = 8.1 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 712 26 None -23 4 Human 7.3 pKi = 7.3 Binding
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 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
16132265 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
3633 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
4931 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
CHEMBL1201610 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
DB01285 274 0 None -5 5 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774675
11993702 3536 18 None -3 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
5416 3536 18 None -3 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
9272 3536 18 None -3 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
CHEMBL3301624 3536 18 None -3 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
DB11700 3536 18 None -3 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19646498
1325 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
1325 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
1325 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
6440621 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
6440621 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
6440621 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
9898183 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
9898183 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
9898183 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
CHEMBL3422426 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
CHEMBL3422426 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12007532
CHEMBL3422426 3543 12 None -5 7 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7658432
1325 3543 12 None -12 7 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
6440621 3543 12 None -12 7 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
9898183 3543 12 None -12 7 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL3422426 3543 12 None -12 7 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1320 363 0 None 3 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
1320 363 0 None 3 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16162729 363 0 None 3 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
16162729 363 0 None 3 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1323 2649 49 None -72 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
92432 2649 49 None -72 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL430239 2649 49 None -72 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
1324 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16154396 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16197727 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
44285019 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
57514683 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
91898441 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
CHEMBL441738 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
DB04931 299 23 None -2 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100