Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1323 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
1323 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 38 Human Functional pEC50 = 10.2 10.2 -54 7
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
CHEMBL413212 215515 None 0 Human Functional pEC50 = 10.2 10.2 -3 4
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
1324 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16154396 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16197727 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
16197727.0 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
44285019 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
57514683 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
91898441 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
CHEMBL441738 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None None 10.1021/jm030452x
DB04931 302 None 19 Rat Functional pEC50 = 10 10.0 -1 8
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 191055 None 0 Human Functional pEC50 = 10.0 10.0 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 191055 None 0 Human Functional pEC50 = 10.0 10.0 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168281421 191066 None 0 Human Functional pEC50 = 10.0 10.0 10 3
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 191066 None 0 Human Functional pEC50 = 10.0 10.0 10 3
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727.0 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 302 None 19 Human Functional pEC50 = 9.9 9.9 -15 8
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
11993702 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 20 Human Functional pEC50 = 9.8 9.8 1 5
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 190194 None 0 Human Functional pEC50 = 9.8 9.8 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 190194 None 0 Human Functional pEC50 = 9.8 9.8 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
168289404 191421 None 0 Human Functional pEC50 = 9.7 9.7 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 191421 None 0 Human Functional pEC50 = 9.7 9.7 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL428615 215921 None 0 Human Functional pEC50 = 9.7 9.7 -10 5
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
1323 2688 None 38 Human Functional pEC50 = 9.7 9.7 -54 7
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 38 Human Functional pEC50 = 9.7 9.7 -54 7
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.7 9.7 -54 7
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
168284733 191733 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 191733 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL405087 215001 None 0 Rat Functional pEC50 = 9.6 9.6 -2 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL414965 215626 None 0 Rat Functional pEC50 = 9.6 9.6 -4 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1324 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 19 Human Functional pEC50 = 9.6 9.6 -15 8
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
1323 2688 None 38 Human Functional pEC50 = 9.6 9.6 -54 7
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 38 Human Functional pEC50 = 9.6 9.6 -54 7
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.6 9.6 -54 7
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
168272660 190542 None 0 Human Functional pEC50 = 9.6 9.6 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 190542 None 0 Human Functional pEC50 = 9.6 9.6 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 19 Human Functional pEC50 = 9.5 9.5 -15 8
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 190064 None 0 Human Functional pEC50 = 9.5 9.5 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 190064 None 0 Human Functional pEC50 = 9.5 9.5 -2 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168276507 190374 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 190374 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16157270 215013 None 15 Human Functional pEC50 = 9.5 9.5 22 6
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 215013 None 15 Human Functional pEC50 = 9.5 9.5 22 6
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 215013 None 15 Human Functional pEC50 = 9.5 9.5 22 6
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 215013 None 15 Human Functional pEC50 = 9.5 9.5 22 6
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 192275 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 192275 None 0 Human Functional pEC50 = 9.5 9.5 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289457 191489 None 0 Human Functional pEC50 = 9.5 9.5 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 191489 None 0 Human Functional pEC50 = 9.5 9.5 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL413912 215560 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.07.046
1324 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16154396 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727.0 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
44285019 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
57514683 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
91898441 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
DB04931 302 None 19 Human Functional pEC50 = 9.4 9.4 -15 8
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
168281389 191031 None 0 Human Functional pEC50 = 9.4 9.4 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 191031 None 0 Human Functional pEC50 = 9.4 9.4 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
1323 2688 None 38 Human Functional pEC50 = 9.4 9.4 -54 7
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
92432 2688 None 38 Human Functional pEC50 = 9.4 9.4 -54 7
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.4 9.4 -54 7
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
44415913 79982 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 79982 None 0 Human Functional pEC50 = 9.4 9.4 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416057 81222 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 81222 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
168295726 192514 None 0 Human Functional pEC50 = 9.2 9.2 -6 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 192514 None 0 Human Functional pEC50 = 9.2 9.2 -6 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16132144 211738 None 29 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
16133793 211738 None 29 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
44273719 211738 None 29 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.2 9.2 -7 8
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
10408 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
10408 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 23 Human Functional pEC50 = 9.2 9.2 -5 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL408257 215164 None 0 Human Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL None None None CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
168283616 191348 None 0 Human Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 191348 None 0 Human Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
42630327 155961 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155961 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
1324 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727.0 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1324 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 19 Human Functional pEC50 = 9.1 9.1 -15 8
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
168271237 190597 None 0 Human Functional pEC50 = 9.0 9.0 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 190597 None 0 Human Functional pEC50 = 9.0 9.0 -3 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44415914 139357 None 0 Human Functional pEC50 = 9 9.0 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 139357 None 0 Human Functional pEC50 = 9 9.0 -5 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
145966364 164215 None 0 Human Functional pEC50 = 9 9.0 3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 164215 None 0 Human Functional pEC50 = 9 9.0 3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
16132144 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16133793 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
44273719 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16132144 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16133793 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
44273719 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16132144 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
16133793 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44273719 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.0 9.0 -7 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL428801 215933 None 0 Human Functional pEC50 = 9.0 9.0 -26 5
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL5090946 217775 None 0 Human Functional pEC50 = 8.9 8.9 -12 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL263822 213049 None 0 Human Functional pEC50 = 8.9 8.9 5 4
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL5087859 217613 None 0 Human Functional pEC50 = 8.9 8.9 4 3
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845450 138556 None 0 Human Functional pEC50 = 8.9 8.9 -28 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 138556 None 0 Human Functional pEC50 = 8.9 8.9 -28 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
16132144 211738 None 29 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
16133793 211738 None 29 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
44273719 211738 None 29 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.9 8.9 -7 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00796-0
CHEMBL5083551 217358 None 0 Human Functional pEC50 = 8.8 8.8 -25 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3600920 214283 None 0 Human Functional pEC50 = 8.8 8.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 38 Human Functional pEC50 = 8.8 8.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 38 Human Functional pEC50 = 8.8 8.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.8 8.8 -54 7
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
CHEMBL439691 216309 None 0 Human Functional pEC50 = 8.8 8.8 5 3
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438030 216205 None 0 Human Functional pEC50 = 8.8 8.8 21 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL267900 213196 None 0 Human Functional pEC50 = 8.8 8.8 -5 2
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
145971389 164728 None 0 Human Functional pEC50 = 8.7 8.7 2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164728 None 0 Human Functional pEC50 = 8.7 8.7 2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
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 214922 None 0 Human Functional pEC50 = 8.7 8.7 -6 4
Effect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
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 164752 None 0 Human Functional pEC50 = 8.7 8.7 11 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164752 None 0 Human Functional pEC50 = 8.7 8.7 11 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -54 7
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 214676 None 1 Human Functional pEC50 = 8.7 8.7 25 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
44416106 141533 None 0 Human Functional pEC50 = 8 8.0 -19 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 141533 None 0 Human Functional pEC50 = 8 8.0 -19 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44413830 77979 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209622 77979 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
24774358 154994 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL400866 154994 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
137638725 157071 None 0 Human Functional pEC50 = 6 6.0 -38 3
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4073016 157071 None 0 Human Functional pEC50 = 6 6.0 -38 3
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137660671 159311 None 0 Human Functional pEC50 = 6 6.0 -1071 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 159311 None 0 Human Functional pEC50 = 6 6.0 -1071 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL411359 215339 None 0 Human Functional pEC50 = 6 6.0 -4 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44441645 94180 None 0 Human Functional pEC50 = 6 6.0 -93 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 94180 None 0 Human Functional pEC50 = 6 6.0 -93 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44394660 67075 None 0 Human Functional pEC50 = 6.0 6.0 -70 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL187167 67075 None 0 Human Functional pEC50 = 6.0 6.0 -70 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394654 124040 None 0 Human Functional pEC50 = 6.0 6.0 -26 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL362879 124040 None 0 Human Functional pEC50 = 6.0 6.0 -26 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25132866 172714 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL449131 172714 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
46885761 8030 None 0 Human Functional pEC50 = 5.0 5.0 -173 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL1090813 8030 None 0 Human Functional pEC50 = 5.0 5.0 -173 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
25133556 188957 None 0 Human Functional pEC50 = 7.0 7.0 -83 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 188957 None 0 Human Functional pEC50 = 7.0 7.0 -83 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
122184635 122500 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122500 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371712 212568 None 0 Human Functional pEC50 = 8.0 8.0 -2 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 8.0 8.0 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5091236 217789 None 0 Human Functional pEC50 = 8.0 8.0 -102 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
25128751 173688 None 0 Human Functional pEC50 = 6.0 6.0 -29 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 173688 None 0 Human Functional pEC50 = 6.0 6.0 -29 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
71459938 79012 None 0 Human Functional pEC50 = 6.0 6.0 -19 4
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 79012 None 0 Human Functional pEC50 = 6.0 6.0 -19 4
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
25128749 178575 None 0 Human Functional pEC50 = 7.0 7.0 -37 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 178575 None 0 Human Functional pEC50 = 7.0 7.0 -37 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL3601426 214286 None 0 Human Functional pEC50 = 6.0 6.0 -24 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
11847001 80259 None 0 Human Functional pEC50 = 6.0 6.0 -125 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 80259 None 0 Human Functional pEC50 = 6.0 6.0 -125 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44441641 94354 None 0 Human Functional pEC50 = 6.9 6.9 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 94354 None 0 Human Functional pEC50 = 6.9 6.9 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
145989222 167376 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 167376 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
11328898 7962 None 25 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 7962 None 25 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1204059 7962 None 25 Human Functional pEC50 = 5.9 5.9 -95 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
46885972 8121 None 0 Human Functional pEC50 = 4.9 4.9 -165 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1091631 8121 None 0 Human Functional pEC50 = 4.9 4.9 -165 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
11845630 139601 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 139601 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
25129453 171869 None 0 Human Functional pEC50 = 7.9 7.9 -15 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 171869 None 0 Human Functional pEC50 = 7.9 7.9 -15 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
145966490 164457 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 164457 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 7.9 7.9 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2370967 212429 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
145980719 166591 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 166591 None 0 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44322957 208669 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 208669 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408189 168982 None 0 Human Functional pEC50 = 5.9 5.9 -107 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168982 None 0 Human Functional pEC50 = 5.9 5.9 -107 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
44413881 137680 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 137680 None 0 Human Functional pEC50 = 5.9 5.9 -4 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
137635422 156000 None 0 Human Functional pEC50 = 6.9 6.9 -30 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 156000 None 0 Human Functional pEC50 = 6.9 6.9 -30 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
172446133 195506 None 0 Human Functional pEC50 = 5.9 5.9 -63 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[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.2c01587
CHEMBL5405038 195506 None 0 Human Functional pEC50 = 5.9 5.9 -63 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[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.2c01587
CHEMBL5093939 217948 None 0 Human Functional pEC50 = 6.9 6.9 -169 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2310901 211957 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44322958 107068 None 0 Human Functional pEC50 = 7.9 7.9 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 107068 None 0 Human Functional pEC50 = 7.9 7.9 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL3600843 214280 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5076315 216916 None 0 Human Functional pEC50 = 7.9 7.9 -8 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL501592 216629 None 0 Human Functional pEC50 = 6.9 6.9 -37 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44322986 106153 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 106153 None 0 Human Functional pEC50 = 6.9 6.9 -18 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
1338 3807 None 36 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Rat Functional pEC50 = 5.9 5.9 -1202 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44394093 127306 None 0 Human Functional pEC50 = 5.9 5.9 -8 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365825 127306 None 0 Human Functional pEC50 = 5.9 5.9 -8 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL217584 211836 None 0 Human Functional pEC50 = 6.9 6.9 -74 3
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
11846673 80025 None 0 Human Functional pEC50 = 5.9 5.9 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 80025 None 0 Human Functional pEC50 = 5.9 5.9 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL500743 216612 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44394786 124147 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363271 124147 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL2096759 211667 None 0 Human Functional pEC50 = 6.9 6.9 -21 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
122184914 122625 None 0 Human Functional pEC50 = 5.9 5.9 -69 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122625 None 0 Human Functional pEC50 = 5.9 5.9 -69 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44422999 168958 None 0 Human Functional pEC50 = 5.9 5.9 -446 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 168958 None 0 Human Functional pEC50 = 5.9 5.9 -446 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
1338 3807 None 36 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 3807 None 36 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 3807 None 36 Human Functional pEC50 = 5.9 5.9 -616 8
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
162669632 182671 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182671 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44416152 81129 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 81129 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394657 127531 None 0 Human Functional pEC50 = 5.8 5.8 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL366040 127531 None 0 Human Functional pEC50 = 5.8 5.8 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394583 122411 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359927 122411 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25129105 177124 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 177124 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
44413968 80260 None 0 Human Functional pEC50 = 5.8 5.8 -77 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 80260 None 0 Human Functional pEC50 = 5.8 5.8 -77 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
137658158 159811 None 0 Human Functional pEC50 = 5.8 5.8 -26 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159811 None 0 Human Functional pEC50 = 5.8 5.8 -26 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
9849434 177035 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL462044 177035 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL184968 211511 None 0 Human Functional pEC50 = 5.8 5.8 -11 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CCC(=O)OC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25133907 176829 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 176829 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44413914 139605 None 0 Human Functional pEC50 = 7.8 7.8 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 139605 None 0 Human Functional pEC50 = 7.8 7.8 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5087814 217609 None 0 Human Functional pEC50 = 7.8 7.8 -12 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44577516 172977 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL451535 172977 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
11273288 12965 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 12965 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL538567 12965 None 0 Human Functional pEC50 = 6.8 6.8 -61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL2370965 212427 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 5.8 5.8 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
162672691 183307 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183307 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672691 183307 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183307 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44448590 95652 None 0 Human Functional pEC50 = 6.8 6.8 -93 3
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95652 None 0 Human Functional pEC50 = 6.8 6.8 -93 3
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600842 214279 None 0 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077144 216973 None 0 Human Functional pEC50 = 7.8 7.8 -38 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 211738 None 29 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
16133793 211738 None 29 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
44273719 211738 None 29 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.8 7.8 -7 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
1323 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
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 156015 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 156015 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
1338 3807 None 36 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 36 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 36 Human Functional pEC50 = 6.8 6.8 -616 8
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
44322923 209004 None 0 Human Functional pEC50 = 6.8 6.8 -19 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 209004 None 0 Human Functional pEC50 = 6.8 6.8 -19 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10325955 165366 None 0 Human Functional pEC50 = 5.8 5.8 -112 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 165366 None 0 Human Functional pEC50 = 5.8 5.8 -112 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL184326 211508 None 0 Human Functional pEC50 = 5.8 5.8 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None COP(=S)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC 10.1016/j.bmcl.2004.07.046
CHEMBL3350396 213938 None 0 Human Functional pEC50 = 6.8 6.8 -281 4
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
137662147 159473 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 159473 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
122184575 122493 None 0 Human Functional pEC50 = 6.8 6.8 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 122493 None 0 Human Functional pEC50 = 6.8 6.8 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
168272615 190496 None 0 Human Functional pEC50 = 6.8 6.8 -31 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 190496 None 0 Human Functional pEC50 = 6.8 6.8 -31 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44416060 81349 None 0 Human Functional pEC50 = 6.8 6.8 -102 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 81349 None 0 Human Functional pEC50 = 6.8 6.8 -102 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394658 168440 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434329 168440 None 0 Human Functional pEC50 = 6.8 6.8 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
171378343 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
Agonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 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]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5423711 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
Agonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 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]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL364359 214382 None 0 Human Functional pEC50 = 5.8 5.8 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NS(=O)(=O)C(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
162665450 182402 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182402 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1323 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.8 7.8 -54 7
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 168181 None 0 Human Functional pEC50 = 7.8 7.8 -33 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 168181 None 0 Human Functional pEC50 = 7.8 7.8 -33 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075712 216882 None 0 Human Functional pEC50 = 7.8 7.8 -125 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44394694 66333 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184895 66333 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183733 211506 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL50056 216607 None 1 Human Functional pEC50 = 6.8 6.8 -15 6
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 211619 None 0 Human Functional pEC50 = 5.8 5.8 -1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
CHEMBL2370968 212430 None 0 Human Functional pEC50 = 5.8 5.8 -63 4
Agonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370968 212430 None 0 Human Functional pEC50 = 5.8 5.8 -63 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
162665450 182402 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182402 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL361252 214294 None 0 Human Functional pEC50 = 6.8 6.8 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CN(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11847312 79793 None 0 Human Functional pEC50 = 5.8 5.8 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 79793 None 0 Human Functional pEC50 = 5.8 5.8 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
122184638 122503 None 0 Human Functional pEC50 = 5.8 5.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 122503 None 0 Human Functional pEC50 = 5.8 5.8 2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5092761 217878 None 0 Human Functional pEC50 = 7.7 7.7 -281 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
10077258 15037 None 0 Human Functional pEC50 = 5.8 5.8 -158 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15037 None 0 Human Functional pEC50 = 5.8 5.8 -158 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
11226756 120038 None 0 Human Functional pEC50 = 5.8 5.8 -251 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 120038 None 0 Human Functional pEC50 = 5.8 5.8 -251 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
122184636 122501 None 0 Human Functional pEC50 = 5.7 5.7 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 122501 None 0 Human Functional pEC50 = 5.7 5.7 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145976444 164058 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 164058 None 0 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL438235 216220 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
137638778 156850 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 156850 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL5090670 217767 None 0 Human Functional pEC50 = 7.7 7.7 -18 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168277258 190819 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 190819 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
168274920 190372 None 0 Human Functional pEC50 = 6.7 6.7 -66 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 190372 None 0 Human Functional pEC50 = 6.7 6.7 -66 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL3601431 214287 None 0 Human Functional pEC50 = 5.7 5.7 -2 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
172457809 196344 None 0 Human Functional pEC50 = 6.7 6.7 -199 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[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.2c01587
CHEMBL5421885 196344 None 0 Human Functional pEC50 = 6.7 6.7 -199 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[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.2c01587
44415919 141675 None 0 Human Functional pEC50 = 8.7 8.7 4 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 141675 None 0 Human Functional pEC50 = 8.7 8.7 4 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL503229 216651 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
44577510 188843 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188843 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL443071 216381 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 8.7 8.7 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL5087839 217610 None 0 Human Functional pEC50 = 8.7 8.7 -2 3
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
10408 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 23 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
1323 2688 None 38 Human Functional pEC50 = 8.6 8.6 -54 7
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 38 Human Functional pEC50 = 8.6 8.6 -54 7
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.6 8.6 -54 7
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
168278271 191224 None 0 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 191224 None 0 Human Functional pEC50 = 8.6 8.6 -5 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16132144 211738 None 29 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
16133793 211738 None 29 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
44273719 211738 None 29 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.6 8.6 -7 8
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
44348200 160290 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 160290 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL266417 213142 None 0 Human Functional pEC50 = 8.6 8.6 -83 6
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
137660993 159541 None 0 Human Functional pEC50 = 7.7 7.7 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 159541 None 0 Human Functional pEC50 = 7.7 7.7 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
118735102 118866 None 0 Human Functional pEC50 = 5.7 5.7 -53 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 118866 None 0 Human Functional pEC50 = 5.7 5.7 -53 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
10257242 15036 None 0 Human Functional pEC50 = 5.7 5.7 -112 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 15036 None 0 Human Functional pEC50 = 5.7 5.7 -112 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
9960253 117013 None 0 Human Functional pEC50 = 5.7 5.7 -25 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 117013 None 0 Human Functional pEC50 = 5.7 5.7 -25 2
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44409240 74460 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 74460 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44415972 79914 None 0 Human Functional pEC50 = 4.7 4.7 -141 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 79914 None 0 Human Functional pEC50 = 4.7 4.7 -141 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
44415956 142043 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 142043 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44409240 74460 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 74460 None 0 Human Functional pEC50 = 4.7 4.7 -457 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
44413832 78094 None 0 Human Functional pEC50 = 4.7 4.7 -38 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210009 78094 None 0 Human Functional pEC50 = 4.7 4.7 -38 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
11845444 80098 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 80098 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413969 80261 None 0 Human Functional pEC50 = 4.7 4.7 -44 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 80261 None 0 Human Functional pEC50 = 4.7 4.7 -44 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44413970 139102 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 139102 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44415956 142043 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 142043 None 0 Human Functional pEC50 = 4.7 4.7 -24 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44394785 124107 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363061 124107 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137631599 156617 None 0 Human Functional pEC50 = 6.7 6.7 -50 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156617 None 0 Human Functional pEC50 = 6.7 6.7 -50 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11845276 80084 None 0 Human Functional pEC50 = 5.7 5.7 -7 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 80084 None 0 Human Functional pEC50 = 5.7 5.7 -7 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
44394695 123225 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361253 123225 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL427629 215818 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
137655905 158920 None 0 Human Functional pEC50 = 5.7 5.7 -51 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158920 None 0 Human Functional pEC50 = 5.7 5.7 -51 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44413828 139380 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 139380 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
25132864 172705 None 0 Human Functional pEC50 = 6.7 6.7 -42 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 172705 None 0 Human Functional pEC50 = 6.7 6.7 -42 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
137634090 156390 None 0 Human Functional pEC50 = 4.7 4.7 -15 5
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 156390 None 0 Human Functional pEC50 = 4.7 4.7 -15 5
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
CHEMBL5081077 217205 None 0 Human Functional pEC50 = 7.6 7.6 -29 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
9867330 97894 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 97894 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44441684 94184 None 0 Human Functional pEC50 = 6.6 6.6 -28 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 94184 None 0 Human Functional pEC50 = 6.6 6.6 -28 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
44323015 111496 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 111496 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11845272 80389 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 80389 None 0 Human Functional pEC50 = 6.6 6.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44394626 65805 None 0 Human Functional pEC50 = 5.6 5.6 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183476 65805 None 0 Human Functional pEC50 = 5.6 5.6 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25132524 176863 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 176863 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
122184637 122502 None 0 Human Functional pEC50 = 5.6 5.6 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 122502 None 0 Human Functional pEC50 = 5.6 5.6 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL409636 215233 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
44397461 126295 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 126295 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2370963 212425 None 0 Human Functional pEC50 = 5.6 5.6 -85 2
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44441685 94185 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249322 94185 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
118735101 118865 None 0 Human Functional pEC50 = 5.6 5.6 -64 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118865 None 0 Human Functional pEC50 = 5.6 5.6 -64 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
168295131 192351 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 192351 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11845440 138759 None 0 Human Functional pEC50 = 5.6 5.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL377778 138759 None 0 Human Functional pEC50 = 5.6 5.6 -23 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL50056 216607 None 1 Human Functional pEC50 = 6.6 6.6 -15 6
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm060384p
1338 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Human Functional pEC50 = 5.6 5.6 -616 8
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44448660 95026 None 0 Human Functional pEC50 = 6.6 6.6 -691 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 95026 None 0 Human Functional pEC50 = 6.6 6.6 -691 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44569175 188930 None 0 Human Functional pEC50 = 7.6 7.6 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 188930 None 0 Human Functional pEC50 = 7.6 7.6 -12 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
1323 2688 None 38 Human Functional pEC50 = 7.6 7.6 -54 7
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
92432 2688 None 38 Human Functional pEC50 = 7.6 7.6 -54 7
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.6 7.6 -54 7
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 215302 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
49862425 15066 None 0 Human Functional pEC50 = 5.6 5.6 -91 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 15066 None 0 Human Functional pEC50 = 5.6 5.6 -91 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL524861 218113 None 0 Human Functional pEC50 = 5.6 5.6 -17 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
145990599 166951 None 0 Human Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 166951 None 0 Human Functional pEC50 = 6.6 6.6 -4 4
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
145980198 166781 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4282109 166781 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
11846669 80308 None 0 Human Functional pEC50 = 6.6 6.6 -18 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 80308 None 0 Human Functional pEC50 = 6.6 6.6 -18 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
44441644 154928 None 0 Human Functional pEC50 = 6.6 6.6 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 154928 None 0 Human Functional pEC50 = 6.6 6.6 -69 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL434357 216113 None 0 Human Functional pEC50 = 5.6 5.6 -19 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None COP(=O)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC 10.1016/j.bmcl.2004.07.046
44413880 77975 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 77975 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
137659790 159416 None 0 Human Functional pEC50 = 5.6 5.6 -11 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 159416 None 0 Human Functional pEC50 = 5.6 5.6 -11 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137653925 158699 None 0 Human Functional pEC50 = 4.6 4.6 -64 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 158699 None 0 Human Functional pEC50 = 4.6 4.6 -64 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL427205 215813 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
24774602 169034 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 169034 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2115441 211727 None 0 Human Functional pEC50 = 7.6 7.6 -144 4
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
25132525 176830 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 176830 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
145971673 164793 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217191 164793 None 0 Human Functional pEC50 = 6.6 6.6 -4 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44323032 209062 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 209062 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162672255 182977 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL383250 214772 None 0 Human Functional pEC50 = 5.6 5.6 -18 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
137659790 159416 None 0 Human Functional pEC50 = 6.6 6.6 -11 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 159416 None 0 Human Functional pEC50 = 6.6 6.6 -11 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44413829 78095 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 78095 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44445082 154391 None 0 Human Functional pEC50 = 7.5 7.5 6 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 154391 None 0 Human Functional pEC50 = 7.5 7.5 6 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
162672255 182977 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
137656521 159838 None 0 Human Functional pEC50 = 6.5 6.5 -12 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 159838 None 0 Human Functional pEC50 = 6.5 6.5 -12 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44391927 13996 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 13996 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL3216393 13996 None 0 Human Functional pEC50 = 5.5 5.5 -57 3
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
168296647 192584 None 0 Human Functional pEC50 = 6.5 6.5 -158 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 192584 None 0 Human Functional pEC50 = 6.5 6.5 -158 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44441648 154781 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 154781 None 0 Human Functional pEC50 = 5.5 5.5 -41 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44413842 138464 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 138464 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44394624 97069 None 0 Human Functional pEC50 = 8.5 8.5 -60 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL266665 97069 None 0 Human Functional pEC50 = 8.5 8.5 -60 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL410404 215279 None 0 Rat Functional pEC50 = 8.5 8.5 -25 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -54 7
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
145966716 164400 None 0 Human Functional pEC50 = 8.5 8.5 18 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 164400 None 0 Human Functional pEC50 = 8.5 8.5 18 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL5094168 217969 None 0 Human Functional pEC50 = 8.5 8.5 -42 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
1334 1501 None 4 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
16133814 1501 None 4 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1501 None 4 Human Functional pEC50 = 8.4 8.4 1 4
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
133053557 163801 None 0 Human Functional pEC50 = 7.5 7.5 6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 163801 None 0 Human Functional pEC50 = 7.5 7.5 6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
137633806 156572 None 0 Human Functional pEC50 = 7.5 7.5 -10 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 156572 None 0 Human Functional pEC50 = 7.5 7.5 -10 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL380638 214731 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
25128748 190100 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 190100 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL413439 215530 None 0 Human Functional pEC50 = 6.5 6.5 -40 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44322924 107168 None 0 Human Functional pEC50 = 6.5 6.5 -42 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316038 107168 None 0 Human Functional pEC50 = 6.5 6.5 -42 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394659 66975 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL186687 66975 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885712 8073 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 8073 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1204061 8073 None 0 Human Functional pEC50 = 5.5 5.5 -169 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL185869 211512 None 0 Human Functional pEC50 = 5.5 5.5 -89 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CCOC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137641398 158408 None 0 Human Functional pEC50 = 6.5 6.5 -416 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 158408 None 0 Human Functional pEC50 = 6.5 6.5 -416 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL411378 215341 None 0 Rat Functional pEC50 = 7.5 7.5 -56 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1 10.1021/jm030452x
172468229 196810 None 0 Human Functional pEC50 = 7.5 7.5 -5 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 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)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5432664 196810 None 0 Human Functional pEC50 = 7.5 7.5 -5 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 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)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c01587
44413938 139026 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 139026 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44394691 122969 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL360598 122969 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145988867 167199 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4289983 167199 None 0 Human Functional pEC50 = 6.5 6.5 -4 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44413831 78093 None 0 Human Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL210008 78093 None 0 Human Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
172447505 195908 None 0 Human Functional pEC50 = 6.5 6.5 -9 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 872 11 11 9 0.5 C#Cc1ccc2c(c1)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL5413092 195908 None 0 Human Functional pEC50 = 6.5 6.5 -9 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 872 11 11 9 0.5 C#Cc1ccc2c(c1)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
122184910 122621 None 0 Human Functional pEC50 = 6.5 6.5 -30 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122621 None 0 Human Functional pEC50 = 6.5 6.5 -30 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 163929 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 163929 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 7.5 7.5 -54 7
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
92432 2688 None 38 Human Functional pEC50 = 7.5 7.5 -54 7
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL430239 2688 None 38 Human Functional pEC50 = 7.5 7.5 -54 7
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 188877 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL505536 188877 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
44394783 126441 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365044 126441 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
172441600 195257 None 0 Human Functional pEC50 = 7.5 7.5 -77 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL5399539 195257 None 0 Human Functional pEC50 = 7.5 7.5 -77 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
44413879 138989 None 0 Human Functional pEC50 = 6.5 6.5 -112 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 138989 None 0 Human Functional pEC50 = 6.5 6.5 -112 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL89270 218389 None 0 Human Functional pEC50 = 6.5 6.5 -11 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1016/s0960-894x(03)00552-3
11753695 8395 None 6 Human Functional pEC50 = 6.5 6.5 -281 7
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 8395 None 6 Human Functional pEC50 = 6.5 6.5 -281 7
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
CHEMBL410168 215264 None 0 Human Functional pEC50 = 7.4 7.4 -4 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
46885523 7805 None 0 Human Functional pEC50 = 5.4 5.4 -512 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
CHEMBL1089461 7805 None 0 Human Functional pEC50 = 5.4 5.4 -512 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
46885711 8072 None 0 Human Functional pEC50 = 5.4 5.4 -123 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 8072 None 0 Human Functional pEC50 = 5.4 5.4 -123 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL446185 216405 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
44415912 139313 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 139313 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44408287 75412 None 0 Human Functional pEC50 = 6.4 6.4 -218 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75412 None 0 Human Functional pEC50 = 6.4 6.4 -218 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL2371962 212618 None 0 Human Functional pEC50 = 6.4 6.4 -1412 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
11845804 79589 None 0 Human Functional pEC50 = 5.4 5.4 -467 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL211419 79589 None 0 Human Functional pEC50 = 5.4 5.4 -467 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5094215 217971 None 0 Human Functional pEC50 = 7.4 7.4 -46 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
168285904 191779 None 0 Human Functional pEC50 = 6.4 6.4 -234 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 191779 None 0 Human Functional pEC50 = 6.4 6.4 -234 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL263878 213057 None 0 Human Functional pEC50 = 7.4 7.4 2 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
168290510 192006 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 192006 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
172441036 195202 None 0 Human Functional pEC50 = 7.4 7.4 -79 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[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.2c01587
CHEMBL5398659 195202 None 0 Human Functional pEC50 = 7.4 7.4 -79 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[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.2c01587
CHEMBL5085972 217492 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL91957 218395 None 0 Human Functional pEC50 = 6.4 6.4 -35 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
122184909 122620 None 0 Human Functional pEC50 = 5.4 5.4 -13 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122620 None 0 Human Functional pEC50 = 5.4 5.4 -13 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077811 217004 None 0 Human Functional pEC50 = 6.4 6.4 -72 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL5080489 217177 None 0 Human Functional pEC50 = 8.4 8.4 -4 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
145976863 163853 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163853 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1324 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960845e
1324 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 19 Human Functional pEC50 = 8.4 8.4 -15 8
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 216286 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44394623 141625 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL384720 141625 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322896 168075 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 168075 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25133210 169560 None 0 Human Functional pEC50 = 7.4 7.4 -44 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 169560 None 0 Human Functional pEC50 = 7.4 7.4 -44 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
44322787 106020 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 106020 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162669632 182671 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182671 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL409049 215205 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44347927 157368 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 157368 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
16007263 79827 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 79827 None 0 Human Functional pEC50 = 7.4 7.4 -23 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394784 126363 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365019 126363 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885526 7766 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
CHEMBL1089135 7766 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
CHEMBL1204056 7766 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
44413931 78044 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 78044 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
145948876 167581 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 167581 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44394693 96651 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263234 96651 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL382369 214765 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
44441647 154780 None 0 Human Functional pEC50 = 6.4 6.4 -18 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399714 154780 None 0 Human Functional pEC50 = 6.4 6.4 -18 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
168278924 191175 None 0 Human Functional pEC50 = 6.4 6.4 -22 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 191175 None 0 Human Functional pEC50 = 6.4 6.4 -22 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
44569176 172648 None 0 Human Functional pEC50 = 7.4 7.4 -48 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 172648 None 0 Human Functional pEC50 = 7.4 7.4 -48 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
25129107 173881 None 0 Human Functional pEC50 = 7.4 7.4 -36 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 173881 None 0 Human Functional pEC50 = 7.4 7.4 -36 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL184870 211510 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None C=CCNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322959 156166 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 156166 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408154 141449 None 0 Human Functional pEC50 = 6.4 6.4 -316 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 141449 None 0 Human Functional pEC50 = 6.4 6.4 -316 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
44322788 157475 None 0 Human Functional pEC50 = 6.4 6.4 -58 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 157475 None 0 Human Functional pEC50 = 6.4 6.4 -58 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394690 124715 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL364119 124715 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168285101 191753 None 0 Human Functional pEC50 = 6.3 6.3 -213 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191753 None 0 Human Functional pEC50 = 6.3 6.3 -213 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
46885760 8280 None 0 Human Functional pEC50 = 5.3 5.3 -102 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
CHEMBL1092550 8280 None 0 Human Functional pEC50 = 5.3 5.3 -102 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
44394582 168477 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434544 168477 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL3600840 214277 None 0 Human Functional pEC50 = 6.3 6.3 -1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
137641157 157156 None 0 Human Functional pEC50 = 6.3 6.3 -131 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 157156 None 0 Human Functional pEC50 = 6.3 6.3 -131 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44394581 122215 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359702 122215 None 0 Human Functional pEC50 = 6.3 6.3 -12 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885482 8332 None 0 Human Functional pEC50 = 6.3 6.3 -81 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092860 8332 None 0 Human Functional pEC50 = 6.3 6.3 -81 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44394580 122214 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359701 122214 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145972289 164615 None 0 Human Functional pEC50 = 8.3 8.3 27 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 164615 None 0 Human Functional pEC50 = 8.3 8.3 27 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
92432 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
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 156071 None 0 Human Functional pEC50 = 8.3 8.3 -15 3
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 156071 None 0 Human Functional pEC50 = 8.3 8.3 -15 3
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
1323 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
1323 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.3 8.3 -54 7
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
172445559 195459 None 0 Human Functional pEC50 = 8.3 8.3 -3 4
Agonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[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/acs.jmedchem.2c01794
CHEMBL5404193 195459 None 0 Human Functional pEC50 = 8.3 8.3 -3 4
Agonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[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/acs.jmedchem.2c01794
CHEMBL405791 215040 None 0 Rat Functional pEC50 = 8.3 8.3 -1 4
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ncc[nH]2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL2372570 212730 None 0 Human Functional pEC50 = 8.3 8.3 -53 4
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O 10.1021/jm9017866
44415920 80402 None 0 Human Functional pEC50 = 8.3 8.3 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 80402 None 0 Human Functional pEC50 = 8.3 8.3 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
1334 1501 None 4 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 4 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 4 Human Functional pEC50 = 8.2 8.2 1 4
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm000211e
44577515 189115 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 189115 None 0 Human Functional pEC50 = 7.3 7.3 2 2
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
172468014 196563 None 0 Human Functional pEC50 = 7.3 7.3 -31 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 934 11 13 11 -0.4 C[C@H]1NC(=O)c2cc(N)ccc2SC[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.2c01587
CHEMBL5426684 196563 None 0 Human Functional pEC50 = 7.3 7.3 -31 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 934 11 13 11 -0.4 C[C@H]1NC(=O)c2cc(N)ccc2SC[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.2c01587
46885415 8281 None 0 Human Functional pEC50 = 6.3 6.3 -15 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092571 8281 None 0 Human Functional pEC50 = 6.3 6.3 -15 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
168277543 190784 None 0 Human Functional pEC50 = 6.3 6.3 -125 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 190784 None 0 Human Functional pEC50 = 6.3 6.3 -125 4
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44577510 188843 None 0 Human Functional pEC50 = 5.3 5.3 -3 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
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/acs.jmedchem.2c01587
CHEMBL504986 188843 None 0 Human Functional pEC50 = 5.3 5.3 -3 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
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/acs.jmedchem.2c01587
25129109 188809 None 0 Human Functional pEC50 = 7.3 7.3 -30 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 188809 None 0 Human Functional pEC50 = 7.3 7.3 -30 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
122184911 122622 None 0 Human Functional pEC50 = 5.3 5.3 -10 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122622 None 0 Human Functional pEC50 = 5.3 5.3 -10 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
118735099 118863 None 0 Human Functional pEC50 = 7.3 7.3 -4 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 118863 None 0 Human Functional pEC50 = 7.3 7.3 -4 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
25133209 173455 None 0 Human Functional pEC50 = 7.3 7.3 -19 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 173455 None 0 Human Functional pEC50 = 7.3 7.3 -19 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
1334 1501 None 4 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.3 6.3 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
137636965 156307 None 0 Human Functional pEC50 = 5.3 5.3 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 156307 None 0 Human Functional pEC50 = 5.3 5.3 -13 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44408173 75427 None 0 Human Functional pEC50 = 6.3 6.3 -186 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75427 None 0 Human Functional pEC50 = 6.3 6.3 -186 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44413876 79775 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 79775 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 79775 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 79775 None 0 Human Functional pEC50 = 6.3 6.3 -93 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
25132526 189031 None 0 Human Functional pEC50 = 6.3 6.3 -69 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
CHEMBL507876 189031 None 0 Human Functional pEC50 = 6.3 6.3 -69 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
118735103 118867 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118867 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44408253 140431 None 0 Human Functional pEC50 = 6.3 6.3 -54 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 140431 None 0 Human Functional pEC50 = 6.3 6.3 -54 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL183315 211502 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394734 64578 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181494 64578 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44577520 188932 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 188932 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL5078687 217068 None 0 Human Functional pEC50 = 7.3 7.3 -25 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44413913 138760 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 138760 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
145988152 167140 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 167140 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
46885759 8278 None 0 Human Functional pEC50 = 6.2 6.2 -95 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092548 8278 None 0 Human Functional pEC50 = 6.2 6.2 -95 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
44322994 107053 None 0 Human Functional pEC50 = 6.2 6.2 -60 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315258 107053 None 0 Human Functional pEC50 = 6.2 6.2 -60 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25129108 172799 None 0 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL450236 172799 None 0 Human Functional pEC50 = 7.2 7.2 -6 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
44322977 111632 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 111632 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11061068 31300 None 0 Human Functional pEC50 = 7.2 7.2 -138 3
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 31300 None 0 Human Functional pEC50 = 7.2 7.2 -138 3
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL2372365 212683 None 0 Rat Functional pEC50 = 7.2 7.2 -1 3
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC(C)(C)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
44408155 140640 None 0 Human Functional pEC50 = 6.2 6.2 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140640 None 0 Human Functional pEC50 = 6.2 6.2 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44413932 137633 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 137633 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
44415918 141636 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 141636 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44275650 94107 None 0 Human Functional pEC50 = 8.2 8.2 -15 4
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 94107 None 0 Human Functional pEC50 = 8.2 8.2 -15 4
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
44322895 163465 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 163465 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370964 212426 None 0 Human Functional pEC50 = 8.2 8.2 -47 4
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 212426 None 0 Human Functional pEC50 = 8.2 8.2 -47 4
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL5080784 217194 None 0 Human Functional pEC50 = 8.2 8.2 -9 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090285 217743 None 0 Human Functional pEC50 = 8.2 8.2 -8 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16133793 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
44273719 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16132144 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
16133793 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44273719 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.2 8.2 -7 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
1324 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16154396 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727.0 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
44285019 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
57514683 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
91898441 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
DB04931 302 None 19 Human Functional pEC50 = 8.2 8.2 -15 8
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
162670951 182944 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
46885558 7811 None 0 Human Functional pEC50 = 6.2 6.2 -151 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089483 7811 None 0 Human Functional pEC50 = 6.2 6.2 -151 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
162670951 182944 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL509582 218036 None 0 Human Functional pEC50 = 6.2 6.2 -16 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
172449425 195974 None 0 Human Functional pEC50 = 7.2 7.2 -467 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[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.2c01587
CHEMBL5414451 195974 None 0 Human Functional pEC50 = 7.2 7.2 -467 4
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[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.2c01587
137637656 156329 None 0 Human Functional pEC50 = 6.2 6.2 -69 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 156329 None 0 Human Functional pEC50 = 6.2 6.2 -69 3
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL411400 215343 None 0 Rat Functional pEC50 = 7.2 7.2 -457 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O 10.1021/jm030452x
44408275 75446 None 0 Human Functional pEC50 = 6.2 6.2 -120 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75446 None 0 Human Functional pEC50 = 6.2 6.2 -120 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44323034 208988 None 0 Human Functional pEC50 = 6.2 6.2 -46 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 208988 None 0 Human Functional pEC50 = 6.2 6.2 -46 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394735 123382 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361578 123382 None 0 Human Functional pEC50 = 6.2 6.2 -34 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168273822 190679 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 190679 None 0 Human Functional pEC50 = 6.2 6.2 -61 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
46885481 7757 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089104 7757 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL415200 215639 None 0 Rat Functional pEC50 = 6.2 6.2 -77 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL184644 211509 None 0 Human Functional pEC50 = 5.2 5.2 -16 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394736 123383 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361579 123383 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11846844 140166 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 140166 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44441642 154494 None 0 Human Functional pEC50 = 6.2 6.2 -77 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 154494 None 0 Human Functional pEC50 = 6.2 6.2 -77 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137640703 157189 None 0 Human Functional pEC50 = 5.2 5.2 -1202 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 157189 None 0 Human Functional pEC50 = 5.2 5.2 -1202 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL264190 213067 None 0 Human Functional pEC50 = 8.2 8.2 -3 7
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
CHEMBL264190 213067 None 0 Human Functional pEC50 = 8.2 8.2 -3 7
Agonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC3R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter 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 10.1021/acs.jmedchem.2c01794
CHEMBL406842 215084 None 0 Rat Functional pEC50 = 8.1 8.1 -66 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL5077095 216967 None 0 Human Functional pEC50 = 8.1 8.1 -57 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
172456996 196308 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 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)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5421108 196308 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 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)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c01587
1334 1501 None 4 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.2 6.2 1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
10146211 64350 None 0 Human Functional pEC50 = 5.2 5.2 -2511 3
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 64350 None 0 Human Functional pEC50 = 5.2 5.2 -2511 3
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
122184577 122495 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 122495 None 0 Human Functional pEC50 = 6.2 6.2 -7 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
46885480 7756 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 7756 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44322812 112445 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 112445 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075506 216867 None 0 Human Functional pEC50 = 7.1 7.1 -512 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137647009 157946 None 0 Human Functional pEC50 = 6.1 6.1 -30 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4083755 157946 None 0 Human Functional pEC50 = 6.1 6.1 -30 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
145964837 164442 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 164442 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
137646617 157636 None 0 Human Functional pEC50 = 5.1 5.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 157636 None 0 Human Functional pEC50 = 5.1 5.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46885524 7806 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1089462 7806 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1204054 7806 None 0 Human Functional pEC50 = 5.1 5.1 -354 3
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL406891 215086 None 0 Rat Functional pEC50 = 7.1 7.1 -34 5
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 6.1 6.1 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL3600922 214285 None 0 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44394730 132555 None 0 Human Functional pEC50 = 6.1 6.1 -53 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL369770 132555 None 0 Human Functional pEC50 = 6.1 6.1 -53 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137647538 158054 None 0 Human Functional pEC50 = 6.1 6.1 -1445 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 158054 None 0 Human Functional pEC50 = 6.1 6.1 -1445 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145975465 164044 None 0 Human Functional pEC50 = 7.1 7.1 -6 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 164044 None 0 Human Functional pEC50 = 7.1 7.1 -6 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145964017 164136 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 164136 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
46919520 15144 None 0 Human Functional pEC50 = 6.1 6.1 -549 6
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15144 None 0 Human Functional pEC50 = 6.1 6.1 -549 6
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
162643435 181773 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181773 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 181773 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181773 None 0 Human Functional pEC50 = 7.1 7.1 4 2
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
122184912 122624 None 0 Human Functional pEC50 = 6.1 6.1 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122624 None 0 Human Functional pEC50 = 6.1 6.1 -3 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
49862377 15047 None 0 Human Functional pEC50 = 7.1 7.1 -13 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 15047 None 0 Human Functional pEC50 = 7.1 7.1 -13 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL3600921 214284 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
137648144 157850 None 0 Human Functional pEC50 = 6.1 6.1 -38 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4082585 157850 None 0 Human Functional pEC50 = 6.1 6.1 -38 2
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
11845438 137710 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL375775 137710 None 0 Human Functional pEC50 = 6.1 6.1 -8 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44394627 124148 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363272 124148 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44416135 80215 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 80215 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
25133208 172097 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 172097 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
44441646 154177 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 154177 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL88185 218386 None 0 Human Functional pEC50 = 6.1 6.1 -38 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25133207 173046 None 0 Human Functional pEC50 = 6.1 6.1 -18 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
CHEMBL451694 173046 None 0 Human Functional pEC50 = 6.1 6.1 -18 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
44413930 138735 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 138735 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44394787 166083 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL425348 166083 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181161 211439 None 0 Human Functional pEC50 = 7.1 7.1 -10 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None CNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394585 66787 None 0 Human Functional pEC50 = 6.1 6.1 -63 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL185868 66787 None 0 Human Functional pEC50 = 6.1 6.1 -63 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137636677 156191 None 0 Human Functional pEC50 = 5.1 5.1 -295 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 156191 None 0 Human Functional pEC50 = 5.1 5.1 -295 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11845813 139891 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 139891 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL410217 215268 None 0 Human Functional pEC50 = 7.1 7.1 -38 3
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
44408252 140756 None 0 Human Functional pEC50 = 6.1 6.1 -77 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140756 None 0 Human Functional pEC50 = 6.1 6.1 -77 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862378 15048 None 0 Human Functional pEC50 = 6.1 6.1 -83 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 15048 None 0 Human Functional pEC50 = 6.1 6.1 -83 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
44394584 96623 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263047 96623 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44323029 209639 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 209639 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285801 191590 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 191590 None 0 Human Functional pEC50 = 8.0 8.0 1 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600841 214278 None 0 Human Functional pEC50 = 8 8.0 1 4
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
49862375 15045 None 0 Human Functional pEC50 = 7.1 7.1 -16 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 15045 None 0 Human Functional pEC50 = 7.1 7.1 -16 4
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
163196518 192238 None 3 Human Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 192238 None 3 Human Functional pEC50 = 6.0 6.0 -52 4
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
172461542 196823 None 0 Human Functional pEC50 = 7.0 7.0 -331 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[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.2c01587
CHEMBL5432868 196823 None 0 Human Functional pEC50 = 7.0 7.0 -331 3
Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[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.2c01587
CHEMBL187125 211514 None 0 Human Functional pEC50 = 6.0 6.0 -30 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)Nc1ccco1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448631 95123 None 0 Human Functional pEC50 = 6.0 6.0 -416 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95123 None 0 Human Functional pEC50 = 6.0 6.0 -416 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL359765 214267 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322987 96785 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 96785 None 0 Human Functional pEC50 = 7.0 7.0 -20 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
24774356 94878 None 0 Human Functional pEC50 = 7.0 7.0 8 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253574 94878 None 0 Human Functional pEC50 = 7.0 7.0 8 2
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL5091245 217790 None 0 Human Functional pEC50 = 7.0 7.0 -26 4
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL414778 215616 None 0 Human Functional pEC50 = 6.0 6.0 -154 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44394586 126847 None 0 Human Functional pEC50 = 6.0 6.0 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365385 126847 None 0 Human Functional pEC50 = 6.0 6.0 -13 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448629 167561 None 0 Human Functional pEC50 = 7.0 7.0 -346 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167561 None 0 Human Functional pEC50 = 7.0 7.0 -346 4
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2112008 211685 None 0 Human Functional pEC50 = 7.0 7.0 1 3
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44323033 107208 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 107208 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132867 172601 None 0 Human Functional pEC50 = 6.0 6.0 -38 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 172601 None 0 Human Functional pEC50 = 6.0 6.0 -38 3
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44408276 75534 None 0 Human Functional pEC50 = 6 6.0 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75534 None 0 Human Functional pEC50 = 6 6.0 -134 4
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
6918813 131439 None 2 Human Functional pEC50 = 6 6.0 -144 4
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Functional pEC50 = 6 6.0 -144 4
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44394692 66235 None 0 Human Functional pEC50 = 6 6.0 -33 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184466 66235 None 0 Human Functional pEC50 = 6 6.0 -33 3
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11753695 8395 None 6 Rat Functional pEC50 = 6 6.0 -501 7
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 8395 None 6 Rat Functional pEC50 = 6 6.0 -501 7
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 212430 None 0 Human Functional pIC50 = 8.0 8.0 -63 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370968 212430 None 0 Human Functional pIC50 = 8.0 8.0 -63 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 212426 None 0 Human Functional pIC50 = 8.0 8.0 -47 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
CHEMBL2370964 212426 None 0 Human Functional pIC50 = 8.0 8.0 -47 4
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
162673640 183088 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 183088 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 183088 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 183088 None 0 Human Functional pIC50 = 6 6.0 -20 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677173 183634 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 183634 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677173 183634 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 183634 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162664942 182299 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 182299 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162644475 181911 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 181911 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162644475 181911 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 181911 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
101043845 190501 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 190501 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
101043845 190501 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 190501 None 1 Human Functional pIC50 = 5.7 5.7 -4 2
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
162668987 182696 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182696 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 182696 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182696 None 0 Human Functional pIC50 = 6.6 6.6 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 183420 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 183420 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 183420 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 183420 None 0 Human Functional pIC50 = 6.5 6.5 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162665567 182455 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 182455 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162665567 182455 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 182455 None 0 Human Functional pIC50 = 6.5 6.5 -4 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162672763 183230 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183230 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183230 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183230 None 0 Human Functional pIC50 = 6.5 6.5 -6 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162667953 182643 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 182643 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
162667953 182643 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 182643 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
162675203 183367 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 183367 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675203 183367 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 183367 None 0 Human Functional pIC50 = 5.4 5.4 -10 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
10855168 182012 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 182012 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
10855168 182012 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 182012 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
162673931 183164 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183164 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 183164 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183164 None 0 Human Functional pIC50 = 7.4 7.4 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
101176453 183068 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 183068 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
101176453 183068 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 183068 None 0 Human Functional pIC50 = 7.3 7.3 -660 3
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
162643518 181817 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181817 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 181817 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 181817 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 183566 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 183566 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 183566 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 183566 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183127 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183127 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183127 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183127 None 0 Human Functional pIC50 = 6.2 6.2 -17 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183559 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183559 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183663 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183663 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183663 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183663 None 0 Human Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183559 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183559 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181830 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181830 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181830 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181830 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183159 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183159 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183159 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183159 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1325 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
1325 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 12 Human Functional pIC50 = 7.1 7.1 -125 4
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 182299 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 182299 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL253364 212968 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](N)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44445083 154394 None 0 Human Functional pKd = 9.8 9.8 2 3
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 154394 None 0 Human Functional pKd = 9.8 9.8 2 3
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
122184576 122494 None 0 Human Functional pKd = 9.1 9.1 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 122494 None 0 Human Functional pKd = 9.1 9.1 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2096742 211665 None 0 Human Functional pKd = 8.7 8.7 -3 6
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm070461w
122184635 122500 None 0 Human Functional pKd = 8 8.0 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122500 None 0 Human Functional pKd = 8 8.0 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184633 122498 None 0 Human Functional pKd = 8.5 8.5 -1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 122498 None 0 Human Functional pKd = 8.5 8.5 -1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413573 215535 None 0 Human Functional pKd = 8.4 8.4 1 4
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
44445085 97127 None 0 Human Functional pKd = 8.3 8.3 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 97127 None 0 Human Functional pKd = 8.3 8.3 1 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL266417 213142 None 0 Human Functional pKd = 8.3 8.3 -83 6
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL428801 215933 None 0 Human Functional pKd = 8.3 8.3 -26 5
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL3600912 214281 None 0 Human Functional pKd = 8.2 8.2 -2 4
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
10408 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
5329 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
9941379.0 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
CHEMBL2070241 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
DB11653 720 None 23 Human Functional pEC50 = 8.1 8.1 -5 4
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C None
6546 3075 None 0 Human Functional pIC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17482720
1334 1501 None 4 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
16133814 1501 None 4 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
CHEMBL437050 1501 None 4 Human Functional pIC50 = 8.2 8.2 1 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
1341 3076 None 0 Human Functional pIC50 = 9.7 9.7 -6 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1335 315 None 0 Human Functional pIC50 None 7.7 7.7 -39 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9819197


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1971 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 32 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
216416 111644 None 40 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111644 None 40 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
71496458 115628 None 61 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115628 None 61 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
135409453 3773 None 26 Human Binding pAC50 = 4.9 4.9 - 19
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Binding pAC50 = 4.9 4.9 - 19
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Binding pAC50 = 4.9 4.9 - 19
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
214 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 43 Human Binding pAC50 = 4.9 4.9 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2435 3590 None 59 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 59 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 59 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 59 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 59 Human Binding pAC50 = 4.9 4.9 - 48
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
25181577 78248 None 44 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78248 None 44 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 21 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 21 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 21 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
176 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157.0 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 398 None 47 Human Binding pAC50 = 4.9 4.9 -6 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2351 4301 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4301 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4301 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
1046 205109 None 68 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
CHEMBL614 205109 None 68 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
156419 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
156419.0 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
4212 201135 None 57 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL1417019 201135 None 57 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL58 201135 None 57 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
41684 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
154257 178724 None 43 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178724 None 43 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
104850 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
24826799 10802 None 64 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10802 None 64 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3926 209699 None 30 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 209699 None 30 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 21 Human Binding pAC50 = 4.8 4.8 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
42890 9427 None 34 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9427 None 34 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
11980903 14498 None 13 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14498 None 13 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14498 None 13 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14498 None 13 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5440 28732 None 28 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28732 None 28 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28732 None 28 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28732 None 28 Human Binding pAC50 = 4.8 4.8 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2194 63103 None 64 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
CHEMBL178862 63103 None 64 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 240 2 0 4 4.2 COc1ccc(-c2cc(=S)ss2)cc1 10.1038/s41467-023-40064-9
5328940 100270 None 65 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 100270 None 65 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
1212 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372.0 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1662 None 37 Human Binding pAC50 = 4.7 4.7 - 65
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3380 22798 None 15 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
CHEMBL13280 22798 None 15 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
1427 2013 None 42 Human Binding pAC50 = 4.7 4.7 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 42 Human Binding pAC50 = 4.7 4.7 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 42 Human Binding pAC50 = 4.7 4.7 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 42 Human Binding pAC50 = 4.7 4.7 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 42 Human Binding pAC50 = 4.7 4.7 - 26
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 21 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 21 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 21 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4011 82440 None 34 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82440 None 34 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
2726 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Binding pAC50 = 4.7 4.7 -186 72
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2519 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
2519.0 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
407 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
463 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL113 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
DB00201 779 None 49 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
11626560 203394 None 56 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 203394 None 56 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
11976 920 None 44 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 920 None 44 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467.0 920 None 44 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 920 None 44 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 920 None 44 Human Binding pAC50 = 4.7 4.7 - 23
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
1056 3371 None 67 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2405 3371 None 67 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
77999 3371 None 67 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
CHEMBL121 3371 None 67 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
DB00412 3371 None 67 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2200 20210 None 38 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2200.0 20210 None 38 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 20210 None 38 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 20210 None 38 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
DB08799 20210 None 38 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
25382 9159 None 27 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9159 None 27 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
51755 57422 None 40 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1651990 57422 None 40 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
4236 28104 None 33 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1373 28104 None 33 Human Binding pAC50 = 4.7 4.7 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
103 4153 None 44 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 None 44 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 None 44 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 None 44 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 None 44 Human Binding pAC50 = 4.7 4.7 - 53
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
202 1508 None 46 Human Binding pAC50 = 4.6 4.6 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1508 None 46 Human Binding pAC50 = 4.6 4.6 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1508 None 46 Human Binding pAC50 = 4.6 4.6 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1508 None 46 Human Binding pAC50 = 4.6 4.6 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1508 None 46 Human Binding pAC50 = 4.6 4.6 - 33
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
180 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Binding pAC50 = 4.6 4.6 - 39
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Binding pAC50 = 4.6 4.6 - 15
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
3676 207728 None 62 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 234 5 1 2 2.6 CCN(CC)CC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
CHEMBL79 207728 None 62 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 234 5 1 2 2.6 CCN(CC)CC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
216239 23803 None 71 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1200485 23803 None 71 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1336 23803 None 71 Human Binding pAC50 = 4.6 4.6 - 7
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
2247 505 None 55 Human Binding pAC50 = 4.6 4.6 -147 41
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Binding pAC50 = 4.6 4.6 -147 41
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Binding pAC50 = 4.6 4.6 -147 41
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Binding pAC50 = 4.6 4.6 -147 41
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Binding pAC50 = 4.6 4.6 -147 41
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
26987 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
26987.0 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 949 None 27 Human Binding pAC50 = 4.6 4.6 - 21
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
3149 12618 None 11 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12618 None 11 Human Binding pAC50 = 5.6 5.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Binding pAC50 = 4.6 4.6 - 85
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
4150 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019.0 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 788 None 26 Human Binding pAC50 = 4.6 4.6 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5284550 41735 None 12 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5284550.0 41735 None 12 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41735 None 12 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41735 None 12 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41735 None 12 Human Binding pAC50 = 4.6 4.6 - 9
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
10184665 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
10184665.0 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3991 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
123631 209859 None 72 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 8 1 7 4.3 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL939 209859 None 72 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 8 1 7 4.3 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Binding pAC50 = 4.6 4.6 - 91
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
5282175 14437 None 23 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1200661 14437 None 23 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
11511120 78425 None 58 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL2110732 78425 None 58 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
3191 102913 None 65 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3191.0 102913 None 65 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102913 None 65 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102913 None 65 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
25077405 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
25077405.0 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3902 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
49800011 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
49800011.0 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1201309 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00666 2715 None 0 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
2398 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Binding pAC50 = 4.6 4.6 - 28
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
10184653 11001 None 62 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
CHEMBL1173655 11001 None 62 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
2585 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2585.0 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 None 59 Human Binding pAC50 = 4.5 4.5 - 22
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
30323 62505 None 35 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62505 None 35 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62505 None 35 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2286 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927.0 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 None 36 Human Binding pAC50 = 4.5 4.5 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
6436173 55132 None 30 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55132 None 30 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
2713 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 207729 None 57 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
72093 35070 None 5 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35070 None 5 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35070 None 5 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
2018 3007 None 26 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
9941444 3007 None 26 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL3349607 3007 None 26 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB06663 3007 None 26 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
2600 3779 None 53 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Binding pAC50 = 5.2 5.2 - 13
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1209 1658 None 52 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 52 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 52 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 52 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 52 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
1222 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396.0 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1664 None 37 Human Binding pAC50 = 5.2 5.2 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
68617 207985 None 33 Human Binding pAC50 = 5.1 5.1 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 207985 None 33 Human Binding pAC50 = 5.1 5.1 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 207985 None 33 Human Binding pAC50 = 5.1 5.1 - 25
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
1016 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3747 None 45 Human Binding pAC50 = 5.1 5.1 -56 35
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
4746 207349 None 24 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 207349 None 24 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 207349 None 24 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
118422671 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562.0 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301.0 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194.0 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2757 None 41 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
16362 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16362.0 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 None 49 Human Binding pAC50 = 5.0 5.0 - 29
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
100 3805 None 44 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 44 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 44 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 44 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 44 Human Binding pAC50 = 5.0 5.0 - 55
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2274 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917.0 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 None 38 Human Binding pAC50 = 5.0 5.0 - 32
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
1155 1629 None 38 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
3343 1629 None 38 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
557 1629 None 38 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL32800 1629 None 38 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
DB01288 1629 None 38 Human Binding pAC50 = 5 5.0 - 5
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
1324 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16154396 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16197727 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16197727.0 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
44285019 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
57514683 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
91898441 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL441738 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
DB04931 302 None 19 Human Binding pEC50 = 9.9 9.9 -2 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
1323 2688 None 38 Human Binding pEC50 = 9.6 9.6 -48 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
92432 2688 None 38 Human Binding pEC50 = 9.6 9.6 -48 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL430239 2688 None 38 Human Binding pEC50 = 9.6 9.6 -48 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm0303103
16132144 211738 None 29 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303103
16133793 211738 None 29 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303103
44273719 211738 None 29 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303103
CHEMBL214332 211738 None 29 Human Binding pEC50 = 9.2 9.2 -30 4
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0303103
CHEMBL2370154 212260 None 0 Human Binding pEC50 = 8.7 8.7 -1 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
44323211 107074 None 0 Human Binding pEC50 = 6 6.0 - 1
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL315397 107074 None 0 Human Binding pEC50 = 6 6.0 - 1
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44323233 106772 None 0 Human Binding pEC50 = 7.9 7.9 -4 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 106772 None 0 Human Binding pEC50 = 7.9 7.9 -4 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL188738 211518 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190551 211525 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
11038873 171983 None 0 Human Binding pEC50 = 5.8 5.8 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL446941 171983 None 0 Human Binding pEC50 = 5.8 5.8 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
44323020 169099 None 0 Human Binding pEC50 = 7.8 7.8 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 169099 None 0 Human Binding pEC50 = 7.8 7.8 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL188459 211516 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL372237 214632 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
44269189 98391 None 0 Human Binding pEC50 = 5.7 5.7 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL275067 98391 None 0 Human Binding pEC50 = 5.7 5.7 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL373344 214635 None 0 Human Binding pEC50 = 7.6 7.6 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
44269217 30268 None 0 Human Binding pEC50 = 6.6 6.6 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL13910 30268 None 0 Human Binding pEC50 = 6.6 6.6 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL186970 211513 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL191120 211539 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL365262 214497 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
44269214 98547 None 0 Human Binding pEC50 = 5.4 5.4 - 0
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276012 98547 None 0 Human Binding pEC50 = 5.4 5.4 - 0
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL365794 214501 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL370321 214627 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44323212 168822 None 0 Human Binding pEC50 = 4.4 4.4 1 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 168822 None 0 Human Binding pEC50 = 4.4 4.4 1 2
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL190080 211521 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL190953 211536 None 0 Human Binding pEC50 = 5.3 5.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL2371829 212593 None 0 Human Binding pEC50 = 5.3 5.3 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL191063 211538 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL189991 211520 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL190732 211526 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
10260053 168306 None 0 Human Binding pEC50 = 7.2 7.2 4 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 168306 None 0 Human Binding pEC50 = 7.2 7.2 4 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL365913 214503 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
44323234 168159 None 0 Human Binding pEC50 = 7.2 7.2 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 168159 None 0 Human Binding pEC50 = 7.2 7.2 7 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322795 209384 None 0 Human Binding pEC50 = 7.2 7.2 -13 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 209384 None 0 Human Binding pEC50 = 7.2 7.2 -13 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11813437 98582 None 0 Human Binding pEC50 = 5.2 5.2 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276301 98582 None 0 Human Binding pEC50 = 5.2 5.2 - 0
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
44322869 106216 None 0 Human Binding pEC50 = 7.1 7.1 6 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 106216 None 0 Human Binding pEC50 = 7.1 7.1 6 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
46877881 204275 None 0 Human Binding pEC50 = 6.1 6.1 -2 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 204275 None 0 Human Binding pEC50 = 6.1 6.1 -2 3
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL190203 211523 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL1161322 210967 None 0 Human Binding pIC50 = 9.7 9.7 -1 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
44366081 10264 None 0 Human Binding pIC50 = 9.7 9.7 -2 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10264 None 0 Human Binding pIC50 = 9.7 9.7 -2 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 211665 None 0 Human Binding pIC50 = 9.6 9.6 -5 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
CHEMBL500743 216612 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
1324 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None None 10.1021/jm960840h
1324 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 19 Human Binding pIC50 = 8.9 8.9 -2 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
1323 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
1323 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
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 164615 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 164615 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44418421 168696 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL435923 168696 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL393075 214922 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
1323 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
92432 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm070461w
1323 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
92432 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm801300c
1323 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.9 8.9 -48 4
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None None 10.1021/jm0510326
CHEMBL204310 211623 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0510326
122184576 122494 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 122494 None 0 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413573 215535 None 0 Human Binding pIC50 = 8.8 8.8 -1 2
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
CHEMBL428801 215933 None 0 Human Binding pIC50 = 8.7 8.7 -100 3
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
1323 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
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 163801 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 163801 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
118735101 118865 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118865 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL410795 215302 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
118735103 118867 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118867 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44315095 103188 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL307857 103188 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL410217 215268 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
44448629 167561 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167561 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
122184635 122500 None 0 Human Binding pIC50 = 7.0 7.0 1 4
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 122500 None 0 Human Binding pIC50 = 7.0 7.0 1 4
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 163929 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 163929 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44445083 154394 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 154394 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
145948876 167581 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 167581 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161316 210963 None 0 Human Binding pIC50 = 7.0 7.0 -63 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
6918813 131439 None 2 Human Binding pIC50 = 6.0 6.0 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Binding pIC50 = 6.0 6.0 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
24774602 169034 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 169034 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44445085 97127 None 0 Human Binding pIC50 = 7.9 7.9 -2 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 97127 None 0 Human Binding pIC50 = 7.9 7.9 -2 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL425591 215799 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
10304547 168355 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL433764 168355 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL382369 214765 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0510326
44448479 155461 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 155461 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
176 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 47 Human Binding pIC50 = 4.9 4.9 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL373344 214635 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL188459 211516 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL190203 211523 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
122184909 122620 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122620 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL203760 211620 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0510326
122184638 122503 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 122503 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
71449047 78511 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 78511 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
10188529 126849 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL365401 126849 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL3350396 213938 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
145964837 164442 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 164442 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL263822 213049 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL383250 214772 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0510326
CHEMBL2371962 212618 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
122184634 122499 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 122499 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44448660 95026 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 95026 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44449216 95324 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL256286 95324 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600912 214281 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44366171 121358 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 121358 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
127053936 152329 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3968918 152329 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
2247 505 None 55 Human Binding pIC50 = 4.8 4.8 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 55 Human Binding pIC50 = 4.8 4.8 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 55 Human Binding pIC50 = 4.8 4.8 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 55 Human Binding pIC50 = 4.8 4.8 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 55 Human Binding pIC50 = 4.8 4.8 -147 41
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 211513 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
145973975 164752 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164752 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
6918813 131439 None 2 Human Binding pIC50 = 5.8 5.8 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Binding pIC50 = 5.8 5.8 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
71456245 79007 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 79007 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
171378343 196422 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 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]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5423711 196422 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 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]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
122184911 122622 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 122622 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184575 122493 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 122493 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
10282847 123031 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360819 123031 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
5624 32701 None 12 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32701 None 12 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32701 None 12 Human Binding pIC50 = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
57854192 153138 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 153138 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
127053937 149141 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL3942822 149141 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
4189 209380 None 58 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 209380 None 58 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 209380 None 58 Human Binding pIC50 = 4.7 4.7 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
1338 3807 None 36 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Rat Binding pIC50 = 5.7 5.7 - 4
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
16132144 211738 None 29 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
16133793 211738 None 29 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44273719 211738 None 29 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.7 7.7 -30 4
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL3600840 214277 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL1161321 210966 None 0 Human Binding pIC50 = 6.7 6.7 -19 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
44577514 172558 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 172558 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL2112008 211685 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2221249 211902 None 0 Human Binding pIC50 = 6.7 6.7 1 3
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O nan
1016 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 None 45 Human Binding pIC50 = 4.7 4.7 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL365913 214503 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL190427 211524 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL190551 211525 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
1323 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
92432 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL None None None None 10.1021/ml500436s
1323 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
1323 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.7 8.7 -48 4
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 216651 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
172445559 195459 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[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/acs.jmedchem.2c01794
CHEMBL5404193 195459 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[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/acs.jmedchem.2c01794
CHEMBL443071 216381 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
145967155 164338 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4211275 164338 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL502300 216640 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2096742 211665 None 0 Human Binding pIC50 = 8.6 8.6 -5 2
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm801300c
CHEMBL501592 216629 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL3752534 214676 None 1 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161320 210965 None 0 Human Binding pIC50 = 8.6 8.6 12 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
CHEMBL1161323 210968 None 0 Human Binding pIC50 = 8.6 8.6 -5 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
122184637 122502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 122502 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL204263 211622 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
CHEMBL524861 218113 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
1324 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
145975465 164044 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 164044 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
122184910 122621 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 122621 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24774521 154347 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398635 154347 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600832 214273 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
71456219 78778 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 78778 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44396986 67453 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 67453 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44408287 75412 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75412 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
15953838 67291 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 67291 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL539306 67291 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
168282779 191280 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5188894 191280 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600920 214283 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145988152 167140 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 167140 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
127053935 144273 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 144273 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL217305 211832 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/s0960-894x(03)00412-8
122184499 122459 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 122459 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
24774438 94908 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253789 94908 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
9808801 60829 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 60829 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
44408286 140755 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 140755 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
6918813 131439 None 2 Human Binding pIC50 = 5.6 5.6 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Binding pIC50 = 5.6 5.6 - 0
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
168273822 190679 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 190679 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
122184578 122496 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600839 122496 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL217584 211836 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
2726 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 48 Human Binding pIC50 = 4.6 4.6 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
168285801 191590 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 191590 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
44347840 162018 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 162018 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 162018 None 0 Human Binding pIC50 = 7.6 7.6 -17 3
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL2096759 211667 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL2115441 211727 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL380638 214731 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
145976444 164058 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 164058 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3600834 214275 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371966 212622 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL203602 211619 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0510326
CHEMBL381739 214752 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
6918707 104247 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL309807 104247 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
44431512 146012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 146012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL2372588 212731 None 0 Human Binding pIC50 = 6.5 6.5 -316 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
44348144 157914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 157914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44349173 117054 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
CHEMBL338768 117054 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
44448631 95123 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95123 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44448590 95652 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95652 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2371712 212568 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44347838 96696 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL263585 96696 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3600835 214276 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2096742 211665 None 0 Human Binding pIC50 = 8.5 8.5 -5 2
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm070461w
1324 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727.0 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1324 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 19 Human Binding pIC50 = 8.5 8.5 -2 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm030111j
CHEMBL266417 213142 None 0 Human Binding pIC50 = 8.5 8.5 -8 3
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL3600736 214272 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1324 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727.0 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 302 None 19 Human Binding pIC50 = 8.4 8.4 -2 4
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL None None None None 10.1021/jm00018a005
145964017 164136 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 164136 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
16132144 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16133793 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
44273719 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16132144 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
16133793 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44273719 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.5 7.5 -30 4
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL408509 215180 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
168295644 192421 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 192421 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
44348183 97218 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL268094 97218 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44408173 75427 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 75427 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL188738 211518 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
6918849 123030 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360818 123030 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
163196518 192238 None 3 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 192238 None 3 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
24774519 94907 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253788 94907 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2310901 211957 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
54587278 60838 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 60838 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3601426 214286 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
6918276 15618 None 4 Human Binding pIC50 = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 15618 None 4 Human Binding pIC50 = 5.5 5.5 -309 8
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44418430 83287 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218748 83287 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
10077258 15037 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15037 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
3198 207971 None 50 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 207971 None 50 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 207971 None 50 Human Binding pIC50 = 4.4 4.4 -75 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL3600842 214279 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24857886 155338 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402769 155338 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
24858629 197925 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL552520 197925 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44408155 140640 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 140640 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44445082 154391 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 154391 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
54586246 60837 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762008 60837 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL2371967 212623 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
CHEMBL190732 211526 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O 10.1021/jm0490033
CHEMBL2371835 212596 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL365794 214501 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
145973779 164827 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217528 164827 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44577510 188843 None 0 Human Binding pIC50 = 7.4 7.4 -199 3
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 188843 None 0 Human Binding pIC50 = 7.4 7.4 -199 3
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
1334 1501 None 4 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Binding pIC50 = 7.4 7.4 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL1775066 211340 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
44408388 140410 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 140410 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44277696 101259 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 101259 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44277696 101259 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 101259 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL1161318 210964 None 0 Human Binding pIC50 = 7.4 7.4 -79 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
44397220 167400 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 167400 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL3600841 214278 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
15953833 79005 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 79005 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
16725559 95042 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 95042 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
44431513 145897 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391704 145897 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
44348200 160290 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 160290 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3348530 213861 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1016/j.bmcl.2003.10.056
CHEMBL2371965 212621 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL439691 216309 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
168296790 192455 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5206941 192455 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
168273291 190641 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179637 190641 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
145987870 167330 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4292317 167330 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44408190 96976 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 96976 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL3600833 214274 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
49862378 15048 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 15048 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
71459938 79012 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 79012 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44397455 123910 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL362523 123910 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL417853 215698 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligandInhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligand
ChEMBL None None None C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(03)00164-1
46919520 15144 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15144 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44408276 75534 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 75534 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862425 15066 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 15066 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
44418431 136643 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL373821 136643 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL413439 215530 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
145966716 164400 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 164400 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44431511 88100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL234629 88100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL263948 213058 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960840h
16132144 211738 None 29 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
16133793 211738 None 29 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
44273719 211738 None 29 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
CHEMBL214332 211738 None 29 Human Binding pIC50 = 7.3 7.3 -30 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm960845e
CHEMBL1775062 211339 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2011.03.019
118735100 118864 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 118864 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL191120 211539 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL191063 211538 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL370321 214627 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0490033
CHEMBL3600921 214284 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408252 140756 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140756 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL3600913 214282 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145971389 164728 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164728 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL446185 216405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
71449048 78512 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 78512 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
145966490 164457 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 164457 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145948912 167583 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 167583 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
122184914 122625 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122625 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145966364 164215 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 164215 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3754655 214683 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL414778 215616 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL438920 216270 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL204864 211625 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
16157270 215013 None 15 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 215013 None 15 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL2372589 212732 None 0 Human Binding pIC50 = 8.2 8.2 15 2
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
16157270 215013 None 15 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 215013 None 15 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL427205 215813 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
122184912 122624 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122624 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
44577520 188932 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 188932 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL411359 215339 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
44396987 67214 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL187774 67214 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 79002 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 79002 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71456220 78779 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 78779 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL264190 213067 None 0 Human Binding pIC50 = 7.2 7.2 - 1
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
CHEMBL264190 213067 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter analysisDisplacement of [I125] NDP-alpha-MSH from human MC3R stably overexpressing in HEK293 cells in presence of [I125] labeled NDP-alpha-MSH treated for 40 mins measured by microbeta 2 microplate counter 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 10.1021/acs.jmedchem.2c01794
44408253 140431 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 140431 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL2371963 212619 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL190080 211521 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
168295131 192351 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 192351 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL3600843 214280 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
52918026 60828 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 60828 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
10257242 15036 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 15036 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL3601431 214287 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44408189 168982 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168982 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
168278924 191175 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 191175 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
1334 1501 None 4 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16133814 1501 None 4 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL437050 1501 None 4 Human Binding pIC50 = 7.2 7.2 1 3
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
1334 1501 None 4 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 4 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 4 Human Binding pIC50 = 7.1 7.1 1 3
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None None 10.1021/jm000211e
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
145976863 163853 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163853 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
168274393 190214 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5172938 190214 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
54584302 60832 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 60832 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
54584301 60830 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
CHEMBL1761872 60830 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
44408154 141449 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 141449 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
1338 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
9938402 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL339053 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
1338 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Human Binding pIC50 = 6.1 6.1 -75 4
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
49862375 15045 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 15045 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL190953 211536 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12 10.1021/jm0490033
CHEMBL275999 213285 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O 10.1021/jm0490033
CHEMBL372237 214632 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O 10.1021/jm0490033
122184577 122495 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 122495 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
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 122501 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 122501 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.1 8.1 -48 4
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1021/jm960845e
CHEMBL3349030 213864 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL409144 215207 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm0510326
10210964 67264 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL187990 67264 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
44445084 160833 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL411391 160833 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44408275 75446 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 75446 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL375947 214692 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
49862377 15047 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 15047 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
11753695 8395 None 6 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8395 None 6 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
122184633 122498 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 122498 None 0 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
1323 2688 None 38 Human Binding pIC50 = 8.0 8.0 -48 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
92432 2688 None 38 Human Binding pIC50 = 8.0 8.0 -48 4
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c01848
CHEMBL430239 2688 None 38 Human Binding pIC50 = 8.0 8.0 -48 4
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 166951 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 166951 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44397410 124426 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363740 124426 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
1337 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 5 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
10304776 79010 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2113041 79010 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
10483153 60831 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 60831 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3600922 214285 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL389674 214893 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
44366081 10264 None 0 Human Binding pKd = 9.4 9.4 -2 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 10264 None 0 Human Binding pKd = 9.4 9.4 -2 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2372589 212732 None 0 Human Binding pKd = 9.2 9.2 15 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL1161322 210967 None 0 Human Binding pKd = 9 9.0 -1 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 211665 None 0 Human Binding pKd = 8.7 8.7 -5 2
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0202526
CHEMBL1161320 210965 None 0 Human Binding pKd = 7.6 7.6 12 2
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
CHEMBL1161318 210964 None 0 Human Binding pKd = 6.5 6.5 -79 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
CHEMBL1161321 210966 None 0 Human Binding pKd = 6.4 6.4 -19 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
CHEMBL440801 216330 None 0 Human Binding pKd = 8.3 8.3 -25 2
pA2 against human melanocortin receptor, hMC3RpA2 against human melanocortin receptor, hMC3R
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303103
CHEMBL2096742 211665 None 0 Human Binding pKd = 8.3 8.3 -5 2
pA2 value for the compound against human Melanocortin 3 receptorpA2 value for the compound against human Melanocortin 3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303103
CHEMBL1161323 210968 None 0 Human Binding pKd = 8.2 8.2 -5 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL1161316 210963 None 0 Human Binding pKd = 6.2 6.2 -63 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O 10.1021/jm0202526
CHEMBL2372588 212731 None 0 Human Binding pKd = 6.1 6.1 -316 2
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
162643092 181830 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181830 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 181830 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 181830 None 0 Human Binding pKi = 10.7 10.7 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183159 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183159 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 183159 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 183159 None 0 Human Binding pKi = 10.5 10.5 -1 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183559 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183559 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 183559 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 183559 None 0 Human Binding pKi = 10.5 10.5 -2 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL414718 215611 None 0 Human Binding pKi = 10.0 10.0 -1 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
1325 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
1325 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
6440621 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
9898183 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 3600 None 12 Human Binding pKi = 9.9 9.9 -5 6
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 183164 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183164 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 183164 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 183164 None 0 Human Binding pKi = 9.9 9.9 -8 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL2370968 212430 None 0 Human Binding pKi = 9.7 9.7 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL442504 216377 None 0 Human Binding pKi = 9.6 9.6 -3 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
CHEMBL415165 215636 None 0 Human Binding pKi = 9.6 9.6 -2 5
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
162668987 182696 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182696 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 182696 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 182696 None 0 Human Binding pKi = 9.5 9.5 -15 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183230 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183230 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 183230 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 183230 None 0 Human Binding pKi = 9.5 9.5 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 182977 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 182977 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Binding pKi = 9.4 9.4 -13 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183127 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183127 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 183127 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 183127 None 0 Human Binding pKi = 9.4 9.4 -18 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168277761 190409 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175981 190409 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1324 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16154396 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727.0 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
44285019 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
57514683 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
91898441 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL441738 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
DB04931 302 None 19 Human Binding pKi = 9.2 9.2 -2 4
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
162677133 183663 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183663 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 183663 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 183663 None 0 Human Binding pKi = 9.2 9.2 -19 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
1324 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16154396 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16197727 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
16197727.0 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
44285019 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
57514683 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
91898441 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL441738 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
DB04931 302 None 19 Human Binding pKi = 9.1 9.1 -2 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL2370964 212426 None 0 Human Binding pKi = 9.1 9.1 1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
1323 2688 None 38 Human Binding pKi = 9.0 9.0 -48 4
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
92432 2688 None 38 Human Binding pKi = 9.0 9.0 -48 4
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
CHEMBL430239 2688 None 38 Human Binding pKi = 9.0 9.0 -48 4
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
CHEMBL385465 214811 None 0 Human Binding pKi = 9.0 9.0 -10 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
44415913 79982 None 0 Human Binding pKi = 9 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 79982 None 0 Human Binding pKi = 9 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415914 139357 None 0 Human Binding pKi = 9 9.0 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 139357 None 0 Human Binding pKi = 9 9.0 -1 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415919 141675 None 0 Human Binding pKi = 9.0 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 141675 None 0 Human Binding pKi = 9.0 9.0 -2 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL2370154 212260 None 0 Human Binding pKi = 8.9 8.9 -1 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm020021z
CHEMBL266879 213165 None 0 Human Binding pKi = 8.8 8.8 -6 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0501432
162665450 182402 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182402 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162665450 182402 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 182402 None 0 Human Binding pKi = 8 8.0 -10 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168273645 190434 None 0 Human Binding pKi = 8.0 8.0 -24 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5176443 190434 None 0 Human Binding pKi = 8.0 8.0 -24 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16172929 215461 None 14 Human Binding pKi = 8.0 8.0 -12 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
CHEMBL412536 215461 None 14 Human Binding pKi = 8.0 8.0 -12 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0501432
168289404 191421 None 0 Human Binding pKi = 8.0 8.0 -15 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 191421 None 0 Human Binding pKi = 8.0 8.0 -15 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5087814 217609 None 0 Human Binding pKi = 7 7.0 -26 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44400811 68663 None 0 Human Binding pKi = 6 6.0 -416 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL191857 68663 None 0 Human Binding pKi = 6 6.0 -416 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
9915636 66845 None 0 Human Binding pKi = 6 6.0 -58 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186083 66845 None 0 Human Binding pKi = 6 6.0 -58 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44434860 90076 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238159 90076 None 0 Human Binding pKi = 5 5.0 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL5094168 217969 None 0 Human Binding pKi = 7.0 7.0 -707 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090946 217775 None 0 Human Binding pKi = 7.0 7.0 -75 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44401341 135748 None 0 Human Binding pKi = 5.0 5.0 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL372965 135748 None 0 Human Binding pKi = 5.0 5.0 -3 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
176 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 47 Human Binding pKi = 5.0 5.0 -6 31
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
59149264 76830 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 76830 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 76830 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 76830 None 0 Human Binding pKi = 8.0 8.0 -85 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168277916 190786 None 0 Human Binding pKi = 7.9 7.9 -17 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5181812 190786 None 0 Human Binding pKi = 7.9 7.9 -17 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168272660 190542 None 0 Human Binding pKi = 7.9 7.9 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 190542 None 0 Human Binding pKi = 7.9 7.9 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322869 106216 None 0 Human Binding pKi = 7.0 7.0 6 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 106216 None 0 Human Binding pKi = 7.0 7.0 6 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322895 163465 None 0 Human Binding pKi = 7.0 7.0 -18 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 163465 None 0 Human Binding pKi = 7.0 7.0 -18 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285313 191510 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 191510 None 0 Human Binding pKi = 7.0 7.0 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44433294 153132 None 0 Human Binding pKi = 6.0 6.0 -575 3
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL397580 153132 None 0 Human Binding pKi = 6.0 6.0 -575 3
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL2070254 211644 None 0 Human Binding pKi = 6.0 6.0 -31 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44397030 67390 None 0 Human Binding pKi = 6.0 6.0 -131 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL188651 67390 None 0 Human Binding pKi = 6.0 6.0 -131 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
6918850 125489 None 0 Human Binding pKi = 6.0 6.0 -316 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
CHEMBL364560 125489 None 0 Human Binding pKi = 6.0 6.0 -316 4
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
10270570 89067 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236450 89067 None 0 Human Binding pKi = 5.0 5.0 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44401592 125257 None 0 Human Binding pKi = 6.0 6.0 -4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL364519 125257 None 0 Human Binding pKi = 6.0 6.0 -4 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
46905545 10302 None 0 Human Binding pKi = 5.0 5.0 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161792 10302 None 0 Human Binding pKi = 5.0 5.0 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44415972 79914 None 0 Human Binding pKi = 5.9 5.9 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 79914 None 0 Human Binding pKi = 5.9 5.9 -5 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL5078687 217068 None 0 Human Binding pKi = 5.9 5.9 -75 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845450 138556 None 0 Human Binding pKi = 6.9 6.9 -91 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 138556 None 0 Human Binding pKi = 6.9 6.9 -91 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
51346770 58244 None 0 Human Binding pKi = 5.9 5.9 -10 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
CHEMBL1682209 58244 None 0 Human Binding pKi = 5.9 5.9 -10 4
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
44413876 79775 None 0 Human Binding pKi = 5.9 5.9 -93 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 79775 None 0 Human Binding pKi = 5.9 5.9 -93 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 79775 None 0 Human Binding pKi = 5.9 5.9 -93 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 79775 None 0 Human Binding pKi = 5.9 5.9 -93 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL2370967 212429 None 0 Human Binding pKi = 7.9 7.9 -2 2
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44323234 168159 None 0 Human Binding pKi = 7.9 7.9 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 168159 None 0 Human Binding pKi = 7.9 7.9 7 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347331 16334 None 0 Human Binding pKi = 6.9 6.9 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16334 None 0 Human Binding pKi = 6.9 6.9 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
16007264 79751 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL211564 79751 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
16007264 79751 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
CHEMBL211564 79751 None 0 Human Binding pKi = 5.9 5.9 -63 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
71452732 79065 None 0 Human Binding pKi = 5.9 5.9 -1 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113139 79065 None 0 Human Binding pKi = 5.9 5.9 -1 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
71461657 79070 None 0 Human Binding pKi = 5.9 5.9 -4 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113144 79070 None 0 Human Binding pKi = 5.9 5.9 -4 4
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44435220 89286 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236803 89286 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
10293285 89646 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL237528 89646 None 0 Human Binding pKi = 4.9 4.9 -2 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
10137615 89770 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237692 89770 None 0 Human Binding pKi = 4.9 4.9 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 90064 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90064 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434766 154804 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154804 None 0 Human Binding pKi = 4.9 4.9 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
59149266 76954 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693081 76954 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929807 76954 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070250 76954 None 0 Human Binding pKi = 6.9 6.9 -707 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168296647 192584 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 192584 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
11845813 139891 None 0 Human Binding pKi = 5.9 5.9 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 139891 None 0 Human Binding pKi = 5.9 5.9 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
1338 3807 None 36 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 36 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 36 Human Binding pKi = 6.9 6.9 -75 4
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
44413829 78095 None 0 Human Binding pKi = 5.9 5.9 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 78095 None 0 Human Binding pKi = 5.9 5.9 -10 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
25133556 188957 None 0 Human Binding pKi = 6.9 6.9 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 188957 None 0 Human Binding pKi = 6.9 6.9 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
44569175 188930 None 0 Human Binding pKi = 6.9 6.9 -32 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 188930 None 0 Human Binding pKi = 6.9 6.9 -32 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
168277543 190784 None 0 Human Binding pKi = 4.9 4.9 -128 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 190784 None 0 Human Binding pKi = 4.9 4.9 -128 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
59149255 76956 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 76956 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 76956 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 76956 None 0 Human Binding pKi = 7.9 7.9 -50 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11993702 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 20 Human Binding pKi = 7.9 7.9 -3 5
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
168276507 190374 None 0 Human Binding pKi = 7.9 7.9 -33 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 190374 None 0 Human Binding pKi = 7.9 7.9 -33 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322896 168075 None 0 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 168075 None 0 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168293710 192275 None 0 Human Binding pKi = 7.9 7.9 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 192275 None 0 Human Binding pKi = 7.9 7.9 -56 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322958 107068 None 0 Human Binding pKi = 6.9 6.9 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 107068 None 0 Human Binding pKi = 6.9 6.9 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44432932 87788 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233758 87788 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44400863 69186 None 0 Human Binding pKi = 5.9 5.9 -288 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192464 69186 None 0 Human Binding pKi = 5.9 5.9 -288 3
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44456219 155528 None 0 Human Binding pKi = 5.9 5.9 -275 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL403806 155528 None 0 Human Binding pKi = 5.9 5.9 -275 4
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
16046215 80120 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
CHEMBL213122 80120 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
16046215 80120 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
CHEMBL213122 80120 None 0 Human Binding pKi = 5.9 5.9 -51 4
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
44434843 88734 None 0 Human Binding pKi = 4.9 4.9 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 88734 None 0 Human Binding pKi = 4.9 4.9 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434854 90063 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 90063 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434648 148247 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393558 148247 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
172441600 195257 None 0 Human Binding pKi = 6.9 6.9 -288 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL5399539 195257 None 0 Human Binding pKi = 6.9 6.9 -288 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)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(N)=O)CS2 10.1021/acs.jmedchem.2c01587
168285101 191753 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191753 None 0 Human Binding pKi = 4.9 4.9 -190 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5080489 217177 None 0 Human Binding pKi = 6.9 6.9 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
2247 505 None 55 Human Binding pKi = 4.9 4.9 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 55 Human Binding pKi = 4.9 4.9 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 55 Human Binding pKi = 4.9 4.9 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 55 Human Binding pKi = 4.9 4.9 -147 41
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 55 Human Binding pKi = 4.9 4.9 -147 41
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 71222 None 0 Human Binding pKi = 5.9 5.9 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL195638 71222 None 0 Human Binding pKi = 5.9 5.9 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL420167 215702 None 0 Human Binding pKi = 7.9 7.9 -8 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL266417 213142 None 0 Human Binding pKi = 6.9 6.9 -8 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm010165y
10260053 168306 None 0 Human Binding pKi = 6.9 6.9 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 168306 None 0 Human Binding pKi = 6.9 6.9 4 3
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
44322787 106020 None 0 Human Binding pKi = 6.9 6.9 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 106020 None 0 Human Binding pKi = 6.9 6.9 -12 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370965 212427 None 0 Human Binding pKi = 5.9 5.9 -1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44433439 89958 None 0 Human Binding pKi = 5.9 5.9 -165 3
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL237976 89958 None 0 Human Binding pKi = 5.9 5.9 -165 3
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44323212 168822 None 0 Human Binding pKi = 5.9 5.9 1 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 168822 None 0 Human Binding pKi = 5.9 5.9 1 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
11180881 66842 None 1 Human Binding pKi = 5.9 5.9 -93 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
CHEMBL186074 66842 None 1 Human Binding pKi = 5.9 5.9 -93 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
44395681 66891 None 0 Human Binding pKi = 5.9 5.9 -100 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186289 66891 None 0 Human Binding pKi = 5.9 5.9 -100 4
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44415417 80177 None 0 Human Binding pKi = 5.9 5.9 -12 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL213380 80177 None 0 Human Binding pKi = 5.9 5.9 -12 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
10304463 76802 None 0 Human Binding pKi = 5.9 5.9 -14 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL206840 76802 None 0 Human Binding pKi = 5.9 5.9 -14 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
9915636 66845 None 0 Human Binding pKi = 5.9 5.9 -58 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL186083 66845 None 0 Human Binding pKi = 5.9 5.9 -58 4
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44265715 10187 None 0 Human Binding pKi = 4.9 4.9 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159702 10187 None 0 Human Binding pKi = 4.9 4.9 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
10108894 89771 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
CHEMBL237693 89771 None 0 Human Binding pKi = 4.9 4.9 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
44434697 148781 None 0 Human Binding pKi = 4.9 4.9 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL393994 148781 None 0 Human Binding pKi = 4.9 4.9 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434757 152830 None 0 Human Binding pKi = 4.9 4.9 -7 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397324 152830 None 0 Human Binding pKi = 4.9 4.9 -7 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
25129105 177124 None 0 Human Binding pKi = 6.8 6.8 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 177124 None 0 Human Binding pKi = 6.8 6.8 -23 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL5081077 217205 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
172461542 196823 None 0 Human Binding pKi = 6.8 6.8 -912 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[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.2c01587
CHEMBL5432868 196823 None 0 Human Binding pKi = 6.8 6.8 -912 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[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.2c01587
44401418 124083 None 0 Human Binding pKi = 5.8 5.8 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL362964 124083 None 0 Human Binding pKi = 5.8 5.8 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413913 138760 None 0 Human Binding pKi = 5.8 5.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 138760 None 0 Human Binding pKi = 5.8 5.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL2370963 212425 None 0 Human Binding pKi = 7.8 7.8 -10 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
162670951 182944 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162670951 182944 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Binding pKi = 7.8 7.8 -33 2
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
42630327 155961 None 0 Human Binding pKi = 7.8 7.8 -5 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155961 None 0 Human Binding pKi = 7.8 7.8 -5 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL407809 215145 None 0 Human Binding pKi = 7.8 7.8 -56 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL409049 215205 None 0 Human Binding pKi = 6.8 6.8 -12 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
CHEMBL438235 216220 None 0 Human Binding pKi = 6.8 6.8 1 2
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
44347219 16587 None 0 Human Binding pKi = 6.8 6.8 -301 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 16587 None 0 Human Binding pKi = 6.8 6.8 -301 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
44347105 113409 None 0 Human Binding pKi = 5.8 5.8 -13 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL331728 113409 None 0 Human Binding pKi = 5.8 5.8 -13 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44393441 66450 None 0 Human Binding pKi = 4.8 4.8 -1 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL185195 66450 None 0 Human Binding pKi = 4.8 4.8 -1 4
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434662 88548 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235137 88548 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434781 89938 None 0 Human Binding pKi = 4.8 4.8 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 89938 None 0 Human Binding pKi = 4.8 4.8 -15 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
5624 32701 None 12 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32701 None 12 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32701 None 12 Human Binding pKi = 4.8 4.8 -45 10
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
44413970 139102 None 0 Human Binding pKi = 4.8 4.8 -34 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 139102 None 0 Human Binding pKi = 4.8 4.8 -34 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413938 139026 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 139026 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44569176 172648 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 172648 None 0 Human Binding pKi = 6.8 6.8 -30 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
11846669 80308 None 0 Human Binding pKi = 6.8 6.8 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 80308 None 0 Human Binding pKi = 6.8 6.8 -5 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
168271934 190194 None 0 Human Binding pKi = 7.8 7.8 -9 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 190194 None 0 Human Binding pKi = 7.8 7.8 -9 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
1323 2688 None 38 Human Binding pKi = 7.8 7.8 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 38 Human Binding pKi = 7.8 7.8 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 38 Human Binding pKi = 7.8 7.8 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
44322977 111632 None 0 Human Binding pKi = 6.8 6.8 -2 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 111632 None 0 Human Binding pKi = 6.8 6.8 -2 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44577092 178750 None 0 Human Binding pKi = 6.8 6.8 -144 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467586 178750 None 0 Human Binding pKi = 6.8 6.8 -144 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL427629 215818 None 0 Human Binding pKi = 5.8 5.8 -7 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
24873537 146149 None 0 Human Binding pKi = 5.8 5.8 -138 4
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 146149 None 0 Human Binding pKi = 5.8 5.8 -138 4
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44400661 124406 None 0 Human Binding pKi = 5.8 5.8 -512 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
CHEMBL363641 124406 None 0 Human Binding pKi = 5.8 5.8 -512 2
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
70693083 76957 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929813 76957 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070253 76957 None 0 Human Binding pKi = 5.8 5.8 -6 3
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44434636 89334 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236841 89334 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
9946241 89466 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237079 89466 None 0 Human Binding pKi = 4.8 4.8 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434782 90061 None 0 Human Binding pKi = 4.8 4.8 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238144 90061 None 0 Human Binding pKi = 4.8 4.8 -5 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434693 167443 None 0 Human Binding pKi = 4.8 4.8 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL429451 167443 None 0 Human Binding pKi = 4.8 4.8 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
10211466 169003 None 0 Human Binding pKi = 4.8 4.8 -213 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL438432 169003 None 0 Human Binding pKi = 4.8 4.8 -213 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
4189 209380 None 58 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 209380 None 58 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 209380 None 58 Human Binding pKi = 4.8 4.8 -54 34
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44409257 140673 None 0 Human Binding pKi = 5.8 5.8 -67 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL381357 140673 None 0 Human Binding pKi = 5.8 5.8 -67 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
25133210 169560 None 0 Human Binding pKi = 6.8 6.8 -13 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 169560 None 0 Human Binding pKi = 6.8 6.8 -13 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL427666 215825 None 0 Human Binding pKi = 6.8 6.8 -60 4
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL None None None CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O 10.1021/jm0501432
CHEMBL2221249 211902 None 0 Human Binding pKi = 6.8 6.8 1 3
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O nan
168273045 190363 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5175392 190363 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415920 80402 None 0 Human Binding pKi = 7.8 7.8 -13 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 80402 None 0 Human Binding pKi = 7.8 7.8 -13 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44322959 156166 None 0 Human Binding pKi = 6.8 6.8 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 156166 None 0 Human Binding pKi = 6.8 6.8 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132864 172705 None 0 Human Binding pKi = 6.8 6.8 -12 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 172705 None 0 Human Binding pKi = 6.8 6.8 -12 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
25058412 189549 None 0 Human Binding pKi = 5.8 5.8 -208 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL513404 189549 None 0 Human Binding pKi = 5.8 5.8 -208 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434587 89472 None 0 Human Binding pKi = 5.8 5.8 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237094 89472 None 0 Human Binding pKi = 5.8 5.8 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434848 89002 None 0 Human Binding pKi = 4.8 4.8 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL236443 89002 None 0 Human Binding pKi = 4.8 4.8 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44434690 89340 None 0 Human Binding pKi = 4.8 4.8 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89340 None 0 Human Binding pKi = 4.8 4.8 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434713 89630 None 0 Human Binding pKi = 4.8 4.8 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 89630 None 0 Human Binding pKi = 4.8 4.8 -14 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
10109225 154762 None 0 Human Binding pKi = 4.8 4.8 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL399624 154762 None 0 Human Binding pKi = 4.8 4.8 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44409240 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
CHEMBL202699 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
44409240 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44409240 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 74460 None 0 Human Binding pKi = 5.8 5.8 -16 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
172449425 195974 None 0 Human Binding pKi = 6.8 6.8 -2818 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[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.2c01587
CHEMBL5414451 195974 None 0 Human Binding pKi = 6.8 6.8 -2818 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[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.2c01587
1016 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 None 45 Human Binding pKi = 4.8 4.8 -56 35
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL5075506 216867 None 0 Human Binding pKi = 5.8 5.8 -1348 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137658158 159811 None 0 Human Binding pKi = 4.8 4.8 -63 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159811 None 0 Human Binding pKi = 4.8 4.8 -63 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
1323 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
1323 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 38 Human Binding pKi = 7.7 7.7 -48 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
44396002 124841 None 0 Human Binding pKi = 5.8 5.8 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
CHEMBL364215 124841 None 0 Human Binding pKi = 5.8 5.8 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
11181804 128574 None 0 Human Binding pKi = 5.8 5.8 -158 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 128574 None 0 Human Binding pKi = 5.8 5.8 -158 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
23661656 169147 None 0 Human Binding pKi = 5.8 5.8 -323 5
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 169147 None 0 Human Binding pKi = 5.8 5.8 -323 5
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434661 88547 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL235136 88547 None 0 Human Binding pKi = 4.8 4.8 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
44434603 89947 None 0 Human Binding pKi = 4.8 4.8 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237935 89947 None 0 Human Binding pKi = 4.8 4.8 -2 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265496 97102 None 0 Human Binding pKi = 4.8 4.8 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 97102 None 0 Human Binding pKi = 4.8 4.8 -13 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
44409379 76549 None 0 Human Binding pKi = 4.7 4.7 -85 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL206018 76549 None 0 Human Binding pKi = 4.7 4.7 -85 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
25132525 176830 None 0 Human Binding pKi = 5.7 5.7 -2 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 176830 None 0 Human Binding pKi = 5.7 5.7 -2 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
168270124 190064 None 0 Human Binding pKi = 7.7 7.7 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 190064 None 0 Human Binding pKi = 7.7 7.7 -14 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL407213 215108 None 0 Human Binding pKi = 6.7 6.7 -44 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
44577091 178772 None 0 Human Binding pKi = 6.7 6.7 -56 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467772 178772 None 0 Human Binding pKi = 6.7 6.7 -56 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
10408 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
11490658 64964 None 0 Human Binding pKi = 5.7 5.7 -301 2
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL182277 64964 None 0 Human Binding pKi = 5.7 5.7 -301 2
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL88185 218386 None 0 Human Binding pKi = 5.7 5.7 -11 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11296732 143900 None 0 Human Binding pKi = 5.7 5.7 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL390130 143900 None 0 Human Binding pKi = 5.7 5.7 -43 3
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
10283036 140330 None 0 Human Binding pKi = 5.7 5.7 -331 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380540 140330 None 0 Human Binding pKi = 5.7 5.7 -331 4
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
11296732 143900 None 0 Human Binding pKi = 5.7 5.7 -43 3
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL390130 143900 None 0 Human Binding pKi = 5.7 5.7 -43 3
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44434772 88631 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88631 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434621 146393 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL392094 146393 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
9969456 147705 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393125 147705 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434845 147991 None 0 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393350 147991 None 0 Human Binding pKi = 4.7 4.7 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
71454518 79181 None 0 Human Binding pKi = 4.7 4.7 -12 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL2113315 79181 None 0 Human Binding pKi = 4.7 4.7 -12 4
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
11845444 80098 None 0 Human Binding pKi = 4.7 4.7 -11 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 80098 None 0 Human Binding pKi = 4.7 4.7 -11 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
137631599 156617 None 0 Human Binding pKi = 5.7 5.7 -288 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156617 None 0 Human Binding pKi = 5.7 5.7 -288 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11847001 80259 None 0 Human Binding pKi = 5.7 5.7 -138 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 80259 None 0 Human Binding pKi = 5.7 5.7 -138 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
156010247 177177 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
CHEMBL4633001 177177 None 0 Human Binding pKi = 4.7 4.7 -11 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
10408 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
10408 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 23 Human Binding pKi = 6.7 6.7 -23 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
57646411 76949 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 76949 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57646441 76948 None 0 Human Binding pKi = 8.6 8.6 -20 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 76948 None 0 Human Binding pKi = 8.6 8.6 -20 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL408843 215195 None 0 Human Binding pKi = 8.6 8.6 -6 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL2370533 212327 None 0 Human Binding pKi = 7.7 7.7 -9 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
CHEMBL331259 213820 None 0 Human Binding pKi = 7.7 7.7 -70 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
44323029 209639 None 0 Human Binding pKi = 7.7 7.7 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 209639 None 0 Human Binding pKi = 7.7 7.7 -5 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168284733 191733 None 0 Human Binding pKi = 7.7 7.7 -6 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 191733 None 0 Human Binding pKi = 7.7 7.7 -6 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44577062 193483 None 0 Human Binding pKi = 6.7 6.7 -48 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL525177 193483 None 0 Human Binding pKi = 6.7 6.7 -48 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11296600 123009 None 0 Human Binding pKi = 5.7 5.7 -309 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 123009 None 0 Human Binding pKi = 5.7 5.7 -309 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
10180932 89441 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237051 89441 None 0 Human Binding pKi = 4.7 4.7 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434695 89460 None 0 Human Binding pKi = 4.7 4.7 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237070 89460 None 0 Human Binding pKi = 4.7 4.7 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434766 154804 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 154804 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
25128749 178575 None 0 Human Binding pKi = 6.7 6.7 -25 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 178575 None 0 Human Binding pKi = 6.7 6.7 -25 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
44416152 81129 None 0 Human Binding pKi = 6.7 6.7 -38 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 81129 None 0 Human Binding pKi = 6.7 6.7 -38 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
25129109 188809 None 0 Human Binding pKi = 6.7 6.7 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 188809 None 0 Human Binding pKi = 6.7 6.7 -34 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
44322812 112445 None 0 Human Binding pKi = 6.7 6.7 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 112445 None 0 Human Binding pKi = 6.7 6.7 -4 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434584 152031 None 0 Human Binding pKi = 5.7 5.7 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL396638 152031 None 0 Human Binding pKi = 5.7 5.7 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 88631 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88631 None 0 Human Binding pKi = 4.7 4.7 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434690 89340 None 0 Human Binding pKi = 4.7 4.7 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 89340 None 0 Human Binding pKi = 4.7 4.7 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10291369 169025 None 0 Human Binding pKi = 4.7 4.7 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438672 169025 None 0 Human Binding pKi = 4.7 4.7 -3 3
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
2726 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 48 Human Binding pKi = 4.7 4.7 -186 72
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
25132867 172601 None 0 Human Binding pKi = 6.7 6.7 -6 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 172601 None 0 Human Binding pKi = 6.7 6.7 -6 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44413932 137633 None 0 Human Binding pKi = 6.7 6.7 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 137633 None 0 Human Binding pKi = 6.7 6.7 -4 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL2070244 211643 None 0 Human Binding pKi = 7.7 7.7 -21 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44577093 178751 None 0 Human Binding pKi = 6.7 6.7 -275 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467587 178751 None 0 Human Binding pKi = 6.7 6.7 -275 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
11341045 66187 None 0 Human Binding pKi = 5.7 5.7 -123 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 66187 None 0 Human Binding pKi = 5.7 5.7 -123 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
44434760 88551 None 0 Human Binding pKi = 4.7 4.7 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235140 88551 None 0 Human Binding pKi = 4.7 4.7 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434691 89459 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL237069 89459 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434701 89535 None 0 Human Binding pKi = 4.7 4.7 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL237291 89535 None 0 Human Binding pKi = 4.7 4.7 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
44434778 89777 None 0 Human Binding pKi = 4.7 4.7 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89777 None 0 Human Binding pKi = 4.7 4.7 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434655 90056 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238135 90056 None 0 Human Binding pKi = 4.7 4.7 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 90064 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 90064 None 0 Human Binding pKi = 4.7 4.7 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
168283984 191355 None 0 Human Binding pKi = 6.7 6.7 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190172 191355 None 0 Human Binding pKi = 6.7 6.7 -3 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415956 142043 None 0 Human Binding pKi = 4.7 4.7 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 142043 None 0 Human Binding pKi = 4.7 4.7 -17 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44415956 142043 None 0 Human Binding pKi = 4.7 4.7 -17 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 142043 None 0 Human Binding pKi = 4.7 4.7 -17 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44409103 140210 None 0 Human Binding pKi = 7.6 7.6 -2 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
CHEMBL380120 140210 None 0 Human Binding pKi = 7.6 7.6 -2 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
168283616 191348 None 0 Human Binding pKi = 7.6 7.6 -11 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 191348 None 0 Human Binding pKi = 7.6 7.6 -11 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44323015 111496 None 0 Human Binding pKi = 6.6 6.6 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 111496 None 0 Human Binding pKi = 6.6 6.6 -3 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
23635107 91592 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
CHEMBL240571 91592 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
23635107 91592 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240571 91592 None 0 Human Binding pKi = 6.6 6.6 -81 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11477853 66915 None 0 Human Binding pKi = 5.6 5.6 -63 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 66915 None 0 Human Binding pKi = 5.6 5.6 -63 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
44562414 176922 None 0 Human Binding pKi = 5.6 5.6 -95 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL460942 176922 None 0 Human Binding pKi = 5.6 5.6 -95 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
1338 3807 None 36 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
9938402 3807 None 36 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL339053 3807 None 36 Human Binding pKi = 5.6 5.6 -75 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
44394079 126833 None 0 Human Binding pKi = 5.6 5.6 -85 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL365278 126833 None 0 Human Binding pKi = 5.6 5.6 -85 4
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
9867330 97894 None 0 Human Binding pKi = 5.6 5.6 -100 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 97894 None 0 Human Binding pKi = 5.6 5.6 -100 2
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44397283 67187 None 0 Human Binding pKi = 5.6 5.6 -181 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL187659 67187 None 0 Human Binding pKi = 5.6 5.6 -181 3
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434692 88559 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235176 88559 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434847 88991 None 0 Human Binding pKi = 4.6 4.6 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236442 88991 None 0 Human Binding pKi = 4.6 4.6 -6 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434778 89777 None 0 Human Binding pKi = 4.6 4.6 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 89777 None 0 Human Binding pKi = 4.6 4.6 -27 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434765 161865 None 0 Human Binding pKi = 4.6 4.6 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL413982 161865 None 0 Human Binding pKi = 4.6 4.6 -20 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
137655905 158920 None 0 Human Binding pKi = 4.6 4.6 -64 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158920 None 0 Human Binding pKi = 4.6 4.6 -64 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
16007263 79827 None 0 Human Binding pKi = 6.6 6.6 -41 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 79827 None 0 Human Binding pKi = 6.6 6.6 -41 3
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
24848995 118011 None 0 Human Binding pKi = 7.6 7.6 11 3
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 118011 None 0 Human Binding pKi = 7.6 7.6 11 3
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL263878 213057 None 0 Human Binding pKi = 6.6 6.6 -1 3
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44347331 16334 None 0 Human Binding pKi = 6.6 6.6 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 16334 None 0 Human Binding pKi = 6.6 6.6 -181 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
24180646 148270 None 0 Rat Binding pKi = 6.6 6.6 -338 7
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 148270 None 0 Rat Binding pKi = 6.6 6.6 -338 7
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 127532 None 0 Human Binding pKi = 5.6 5.6 -457 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 127532 None 0 Human Binding pKi = 5.6 5.6 -457 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
44397304 126894 None 0 Human Binding pKi = 5.6 5.6 -199 4
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365465 126894 None 0 Human Binding pKi = 5.6 5.6 -199 4
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434764 88594 None 0 Human Binding pKi = 4.6 4.6 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235358 88594 None 0 Human Binding pKi = 4.6 4.6 -11 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434884 88645 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235617 88645 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434689 89209 None 0 Human Binding pKi = 4.6 4.6 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236649 89209 None 0 Human Binding pKi = 4.6 4.6 -19 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10291370 146054 None 0 Human Binding pKi = 4.6 4.6 -28 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391823 146054 None 0 Human Binding pKi = 4.6 4.6 -28 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434762 153099 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 153099 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44409140 141373 None 0 Human Binding pKi = 5.6 5.6 -10 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL383256 141373 None 0 Human Binding pKi = 5.6 5.6 -10 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
44401386 69546 None 0 Human Binding pKi = 5.6 5.6 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL193409 69546 None 0 Human Binding pKi = 5.6 5.6 -2 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
137636677 156191 None 0 Human Binding pKi = 4.6 4.6 -50 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 156191 None 0 Human Binding pKi = 4.6 4.6 -50 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137636965 156307 None 0 Human Binding pKi = 4.6 4.6 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 156307 None 0 Human Binding pKi = 4.6 4.6 -23 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44409337 170564 None 0 Human Binding pKi = 4.6 4.6 -114 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL444883 170564 None 0 Human Binding pKi = 4.6 4.6 -114 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL2370553 212329 None 0 Human Binding pKi = 7.6 7.6 -16 3
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm010165y
44401440 70144 None 0 Human Binding pKi = 6.6 6.6 -1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL194011 70144 None 0 Human Binding pKi = 6.6 6.6 -1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
11341046 66901 None 0 Human Binding pKi = 5.6 5.6 -95 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 66901 None 0 Human Binding pKi = 5.6 5.6 -95 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
44562440 179147 None 0 Human Binding pKi = 5.6 5.6 -38 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL471340 179147 None 0 Human Binding pKi = 5.6 5.6 -38 3
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
44434880 88644 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235616 88644 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434647 89624 None 0 Human Binding pKi = 4.6 4.6 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
CHEMBL237483 89624 None 0 Human Binding pKi = 4.6 4.6 -4 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
44434767 89769 None 0 Human Binding pKi = 4.6 4.6 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237689 89769 None 0 Human Binding pKi = 4.6 4.6 -17 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434868 149639 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL394669 149639 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434762 153099 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 153099 None 0 Human Binding pKi = 4.6 4.6 -13 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434768 154805 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL399811 154805 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
11308054 133685 None 0 Human Binding pKi = 6.6 6.6 -8 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL371365 133685 None 0 Human Binding pKi = 6.6 6.6 -8 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413914 139605 None 0 Human Binding pKi = 7.6 7.6 -40 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 139605 None 0 Human Binding pKi = 7.6 7.6 -40 3
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
168289457 191489 None 0 Human Binding pKi = 7.6 7.6 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 191489 None 0 Human Binding pKi = 7.6 7.6 -16 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44456222 97978 None 0 Human Binding pKi = 6.6 6.6 -223 3
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 97978 None 0 Human Binding pKi = 6.6 6.6 -223 3
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44323033 107208 None 0 Human Binding pKi = 6.6 6.6 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 107208 None 0 Human Binding pKi = 6.6 6.6 -8 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434694 88635 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235589 88635 None 0 Human Binding pKi = 4.6 4.6 -12 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44434761 89201 None 0 Human Binding pKi = 4.6 4.6 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236626 89201 None 0 Human Binding pKi = 4.6 4.6 -3 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434592 89549 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237315 89549 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434682 148692 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393919 148692 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
172441036 195202 None 0 Human Binding pKi = 6.6 6.6 -1862 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[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.2c01587
CHEMBL5398659 195202 None 0 Human Binding pKi = 6.6 6.6 -1862 3
Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysisDisplacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[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.2c01587
25131477 178806 None 0 Human Binding pKi = 4.6 4.6 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL468252 178806 None 0 Human Binding pKi = 4.6 4.6 -42 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL5075712 216882 None 0 Human Binding pKi = 6.6 6.6 -181 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
57817763 76955 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 76955 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 76955 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 76955 None 0 Human Binding pKi = 7.6 7.6 -338 4
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
23635237 91487 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
CHEMBL240364 91487 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
23635237 91487 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL240364 91487 None 0 Human Binding pKi = 6.6 6.6 -45 3
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
44401513 69184 None 0 Human Binding pKi = 6.6 6.6 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL192450 69184 None 0 Human Binding pKi = 6.6 6.6 1 2
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44434581 167147 None 0 Human Binding pKi = 5.6 5.6 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL428903 167147 None 0 Human Binding pKi = 5.6 5.6 1 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 88631 None 0 Human Binding pKi = 4.6 4.6 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 88631 None 0 Human Binding pKi = 4.6 4.6 -21 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434683 89337 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL236847 89337 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
44434769 89773 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237698 89773 None 0 Human Binding pKi = 4.6 4.6 -16 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434650 89933 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237910 89933 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434651 89934 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237911 89934 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434654 90055 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238134 90055 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434863 148232 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393552 148232 None 0 Human Binding pKi = 4.6 4.6 -10 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168282596 191015 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL5185132 191015 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
168281389 191031 None 0 Human Binding pKi = 7.6 7.6 -7 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 191031 None 0 Human Binding pKi = 7.6 7.6 -7 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
44323233 106772 None 0 Human Binding pKi = 6.6 6.6 -4 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 106772 None 0 Human Binding pKi = 6.6 6.6 -4 2
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322986 106153 None 0 Human Binding pKi = 6.6 6.6 -7 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 106153 None 0 Human Binding pKi = 6.6 6.6 -7 3
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11249545 66225 None 0 Human Binding pKi = 5.6 5.6 -478 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 66225 None 0 Human Binding pKi = 5.6 5.6 -478 4
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11364326 66707 None 0 Human Binding pKi = 5.6 5.6 -134 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 66707 None 0 Human Binding pKi = 5.6 5.6 -134 3
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
24740653 88626 None 0 Human Binding pKi = 5.6 5.6 -758 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL235556 88626 None 0 Human Binding pKi = 5.6 5.6 -758 3
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
44265707 10186 None 0 Human Binding pKi = 4.6 4.6 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159701 10186 None 0 Human Binding pKi = 4.6 4.6 -4 4
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434759 88550 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235139 88550 None 0 Human Binding pKi = 4.6 4.6 -7 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434688 89207 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236640 89207 None 0 Human Binding pKi = 4.6 4.6 -8 4
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168286369 191821 None 0 Human Binding pKi = 6.6 6.6 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5197030 191821 None 0 Human Binding pKi = 6.6 6.6 -4 4
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
137640703 157189 None 0 Human Binding pKi = 4.6 4.6 -218 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 157189 None 0 Human Binding pKi = 4.6 4.6 -218 3
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25133209 173455 None 0 Human Binding pKi = 6.6 6.6 -56 3
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p