Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

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weight		 Rot
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 DOI
127036484 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
1323 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
92432 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL3735690 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL430239 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
127036484 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
1323 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
92432 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL3735690 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL430239 5482 39 None -40 7 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL413212 488271 0 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1058 17 13 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](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
122194229 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
1324 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
16197727 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
4836 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
CHEMBL3629347 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
CHEMBL441738 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
DB04931 621 23 None -1 9 Rat 10.0 pEC50 = 10 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030452x
168284256 374020 0 None -2 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 374020 0 None -2 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 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 374031 0 None 10 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 374031 0 None 10 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
122194229 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
1324 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
16197727 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
4836 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
CHEMBL3629347 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
CHEMBL441738 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
DB04931 621 23 None -9 9 Human 9.9 pEC50 = 9.9 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
11993702 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
DB11700 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
11993702 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
DB11700 484262 27 None 1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
168271934 373182 0 None -1 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 373182 0 None -1 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
168289404 374377 0 None -4 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 374377 0 None -4 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL428615 488519 0 None -10 5 Human 9.7 pEC50 = 9.7 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1042 17 13 11 -1.1 CCCC[C@H](NC(C)=O)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
127036484 5482 39 None -40 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
1323 5482 39 None -40 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
92432 5482 39 None -40 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL3735690 5482 39 None -40 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL430239 5482 39 None -40 7 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
168284733 374685 0 None 1 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 374685 0 None 1 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL405087 487843 0 None -2 5 Rat 9.6 pEC50 = 9.6 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1095 18 14 14 -1.8 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 488377 0 None -4 5 Rat 9.6 pEC50 = 9.6 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1117 18 15 13 -2.5 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
122194229 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
1324 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
16197727 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
4836 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL3629347 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL441738 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
DB04931 621 23 None -9 9 Human 9.6 pEC50 = 9.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
127036484 5482 39 None -40 7 Human 9.6 pEC50 = 9.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
1323 5482 39 None -40 7 Human 9.6 pEC50 = 9.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
92432 5482 39 None -40 7 Human 9.6 pEC50 = 9.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
CHEMBL3735690 5482 39 None -40 7 Human 9.6 pEC50 = 9.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
CHEMBL430239 5482 39 None -40 7 Human 9.6 pEC50 = 9.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
168272660 373521 0 None -2 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 373521 0 None -2 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
122194229 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
1324 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
16197727 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
4836 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL3629347 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
CHEMBL441738 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
DB04931 621 23 None -9 9 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.8b00251
168270124 373056 0 None -2 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 373056 0 None -2 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168276507 373359 0 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 373359 0 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL405282 487855 22 None 104 6 Human 9.5 pEC50 = 9.5 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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 487855 22 None 104 6 Human 9.5 pEC50 = 9.5 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 375204 0 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 375204 0 None -3 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289457 374445 0 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 374445 0 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL413912 488313 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 1646 49 22 21 -4.5 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
122194229 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
1324 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
16197727 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
4836 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
CHEMBL3629347 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
CHEMBL441738 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
DB04931 621 23 None -9 9 Human 9.4 pEC50 = 9.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
168281389 373997 0 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 373997 0 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
127036484 5482 39 None -40 7 Human 9.4 pEC50 = 9.4 Functional
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
1323 5482 39 None -40 7 Human 9.4 pEC50 = 9.4 Functional
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
92432 5482 39 None -40 7 Human 9.4 pEC50 = 9.4 Functional
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL3735690 5482 39 None -40 7 Human 9.4 pEC50 = 9.4 Functional
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL430239 5482 39 None -40 7 Human 9.4 pEC50 = 9.4 Functional
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
44415913 161412 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 161412 0 None -5 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416057 162632 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 162632 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
168295726 375436 0 None -6 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 375436 0 None -6 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL214332 485136 29 None -3 8 Human 9.2 pEC50 = 9.2 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1025 17 13 11 -0.6 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 488005 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL 1174 21 16 15 -3.3 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 374306 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 374306 0 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
42630327 311799 1 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 311799 1 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
122194229 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
1324 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
16197727 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
4836 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL3629347 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL441738 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
DB04931 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
122194229 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
1324 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
16197727 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
4836 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL3629347 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL441738 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
DB04931 621 23 None -9 9 Human 9.1 pEC50 = 9.1 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
168271237 373575 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 373575 0 None -3 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44415914 276593 0 None -5 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 276593 0 None -5 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
145966364 329073 0 None 8 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 329073 0 None 8 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL214332 485136 29 None -3 8 Human 9.0 pEC50 = 9.0 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 485136 29 None -3 8 Human 9.0 pEC50 = 9.0 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 485136 29 None -3 8 Human 9.0 pEC50 = 9.0 Functional
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 488525 0 None -20 5 Human 9.0 pEC50 = 9.0 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1149 17 13 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](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL5090946 479450 0 None -12 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1827 23 24 21 -1.6 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 486104 0 None 144 2 Human 8.9 pEC50 = 8.9 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 886 16 12 9 -1.6 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 479294 0 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1966 27 24 22 -1.2 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](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 270514 0 None -28 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 270514 0 None -28 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL214332 485136 29 None -3 8 Human 8.9 pEC50 = 8.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 479049 0 None -25 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1853 23 23 21 -1.1 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 487205 0 None 186 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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
127036484 5482 39 None -40 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
1323 5482 39 None -40 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
92432 5482 39 None -40 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL3735690 5482 39 None -40 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL430239 5482 39 None -40 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL439691 488789 0 None 21 3 Human 8.8 pEC50 = 8.8 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 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 488691 0 None 21 3 Human 8.8 pEC50 = 8.8 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1551 47 21 18 -3.1 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 486245 0 None -5 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP releaseAgonist activity at human Melanocortin-3 receptor as peptide required for 50% maximal cAMP release
ChEMBL 1174 21 16 15 -3.3 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 329563 0 None 1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 329563 0 None 1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
1323 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
92432 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL3735690 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL430239 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
127036484 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
1323 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
92432 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
CHEMBL3735690 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
CHEMBL430239 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
CHEMBL393075 487766 0 None -6 4 Human 8.7 pEC50 = 8.7 Functional
Effect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1032 16 14 11 -0.1 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
127036484 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
1323 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
92432 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
CHEMBL3735690 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
CHEMBL430239 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
127036484 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
1323 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
92432 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
CHEMBL3735690 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
CHEMBL430239 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
145973975 329587 0 None 7 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 329587 0 None 7 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
1323 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
92432 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
CHEMBL3735690 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
CHEMBL430239 5482 39 None -40 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
CHEMBL3752534 487533 1 None 5 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1131 15 12 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
44416106 278671 0 None -19 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 278671 0 None -19 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44413830 159533 0 None -2 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209622 159533 0 None -2 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
24774358 310913 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL400866 310913 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 811 9 10 8 -0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
137638725 312890 0 None -38 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4073016 312890 0 None -38 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137660671 315069 0 None -1071 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 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 315069 0 None -1071 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 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 488169 0 None -14 4 Human 6.0 pEC50 = 6 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1552 47 21 18 -2.5 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 194541 0 None -34 3 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 194541 0 None -34 3 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44394660 139341 0 None -70 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL187167 139341 0 None -70 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394654 252024 0 None -26 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL362879 252024 0 None -26 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25132866 337125 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL449131 337125 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
46885761 22344 0 None -173 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
CHEMBL1090813 22344 0 None -173 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F 10.1021/jm9017866
25133556 372025 0 None -83 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 372025 0 None -83 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
122184635 241007 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None -10 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2371712 485760 0 None -5 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1588 44 18 19 -0.8 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 486807 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 479464 0 None -102 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1980 28 24 22 -1.1 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 347676 0 None -29 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 347676 0 None -29 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
71459938 160473 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 160473 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
25128749 352383 0 None -37 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 352383 0 None -37 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL3601426 487208 0 None -1412 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 161685 0 None -125 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 161685 0 None -125 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
11061068 64921 0 None -58 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44441641 64921 0 None -58 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL140154 64921 0 None -58 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 64921 0 None -58 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
145989222 332071 0 None -17 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 332071 0 None -17 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
11328898 22276 25 None -95 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 22276 25 None -95 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
DB12517 22276 25 None -95 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
46885972 22435 0 None -165 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1091631 22435 0 None -165 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 3 4.4 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
11845630 270549 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 270549 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
25129453 336297 0 None -15 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 336297 0 None -15 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
145966490 329307 0 None -2 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 329307 0 None -2 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3349030 486807 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 485650 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1612 47 20 18 -1.2 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 331313 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4278563 331313 0 None -3 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 642 17 7 6 1.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44322957 473196 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 473196 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408189 333518 0 None -75 4 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 333518 0 None -75 4 Human 5.9 pEC50 = 5.9 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
44413881 274990 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 274990 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
137635422 311837 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
137636428 311837 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 311837 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4062443 311837 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
172446133 387855 0 None -112 3 Human 5.9 pEC50 = 5.9 Functional
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
172457809 387855 0 None -112 3 Human 5.9 pEC50 = 5.9 Functional
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 387855 0 None -112 3 Human 5.9 pEC50 = 5.9 Functional
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 387855 0 None -112 3 Human 5.9 pEC50 = 5.9 Functional
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 477486 0 None -169 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 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](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 485337 0 None 2 4 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1523 44 18 17 -1.2 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 216665 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 216665 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL3600843 487202 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 478624 0 None -8 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1948 22 21 19 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](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 488985 0 None -426 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1091 16 15 11 -0.9 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]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44322986 215781 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 215781 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10864861 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -2691 9 Rat 5.9 pEC50 = 5.9 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-3 receptor (rMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44394093 255202 0 None -8 3 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365825 255202 0 None -8 3 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL217584 485224 0 None -51 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1095 17 14 12 -1.7 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 161455 0 None -5 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 161455 0 None -5 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL500743 488968 0 None -8 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1041 16 15 11 -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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44394786 252125 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363271 252125 0 None -3 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 883 22 9 7 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL2096759 485069 0 None -17 4 Human 6.9 pEC50 = 6.9 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 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 241132 0 None -54 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 241132 0 None -54 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44422999 333494 0 None -562 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
CHEMBL438118 333494 0 None -562 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1040 15 9 10 3.0 CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm0614275
10864861 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
10886436 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
10952071 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
1338 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL140108 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL334457 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL342954 8293 40 None -1698 9 Human 5.9 pEC50 = 5.9 Functional
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
162669632 356382 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 356382 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44416152 162543 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 162543 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394657 255418 0 None -12 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL366040 255418 0 None -12 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394583 240922 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359927 240922 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25129105 350974 0 None -12 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 350974 0 None -12 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
44413968 161686 0 None -77 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 161686 0 None -77 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
137658158 315551 0 None -26 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 315551 0 None -26 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
9849434 350887 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL462044 350887 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 516 9 2 4 2.8 C=CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL184968 484954 0 None -11 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 787 19 8 8 1.9 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 350684 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 350684 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44413914 270550 0 None -50 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 270550 0 None -50 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5087814 479290 0 None -12 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1859 20 19 19 1.7 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 346997 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL451535 346997 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 908 12 12 12 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
11273288 27222 0 None -75 3 Human 6.8 pEC50 = 6.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 27222 0 None -75 3 Human 6.8 pEC50 = 6.8 Functional
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL2370965 485648 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1586 47 19 17 -0.7 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 486807 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 366554 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 366554 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672691 366554 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 366554 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44448590 195963 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 195963 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600842 487201 0 None 72 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 478676 0 None -38 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1823 25 25 22 -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)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
CHEMBL214332 485136 29 None -3 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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
127036484 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
1323 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
92432 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL3735690 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL430239 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
137637026 311852 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 311852 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
10864861 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
10886436 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
10952071 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
1338 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL140108 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL334457 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL342954 8293 40 None -1698 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
44322923 473504 0 None -19 3 Human 6.8 pEC50 = 6.8 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 473504 0 None -19 3 Human 6.8 pEC50 = 6.8 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10325955 330164 0 None -112 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 330164 0 None -112 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL184326 484951 0 None -3 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 811 21 8 8 2.3 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 486875 0 None -537 4 Human 6.8 pEC50 = 6.8 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1095 17 14 12 -1.7 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 315224 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 315224 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
122184575 241001 0 None -4 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 241001 0 None -4 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
168272615 373477 0 None -31 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 373477 0 None -31 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44416060 162754 0 None -102 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 162754 0 None -102 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394658 333040 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434329 333040 0 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
171378343 388754 0 None -14 4 Human 6.8 pEC50 = 6.8 Functional
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 388754 0 None -14 4 Human 6.8 pEC50 = 6.8 Functional
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 487260 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 19 9 7 1.9 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 356123 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 356123 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
127036484 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
1323 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
92432 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL3735690 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL430239 5482 39 None -40 7 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
44323031 332809 0 None -33 3 Human 7.8 pEC50 = 7.8 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 332809 0 None -33 3 Human 7.8 pEC50 = 7.8 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075712 478591 0 None -125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1924 27 27 22 -2.2 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](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 138605 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184895 138605 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183733 484949 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 832 22 10 8 0.1 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 484368 1 None -15 6 Human 6.8 pEC50 = 6.8 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL203602 485031 0 None -5 3 Human 5.8 pEC50 = 5.8 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 858 15 11 9 -1.4 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 485651 0 None -1380 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC3R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay
ChEMBL 1561 44 19 17 -1.4 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 485651 0 None -1380 4 Human 5.8 pEC50 = 5.8 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1561 44 19 17 -1.4 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 356123 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 356123 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL361252 487216 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 758 18 8 6 1.5 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 161226 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 161226 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
122184638 241010 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 241010 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5092761 479551 0 None -281 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1987 26 22 22 0.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)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 38929 0 None -97 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 38929 0 None -97 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
11226756 238670 0 None -251 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 238670 0 None -251 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
122184636 241008 0 None -13 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 241008 0 None -13 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
145976444 328925 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 328925 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL438235 488705 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1668 35 21 20 -1.9 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 312675 0 None -11 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 312675 0 None -11 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL5090670 479443 0 None -18 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1872 25 25 21 -1.8 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 373793 0 None -39 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 373793 0 None -39 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
178300981 466340 0 None -4 3 Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 432 7 1 3 5.0 CCCN1CC(NC(=O)[C@@H]2C[C@H]2c2cccc(-c3cc(Cl)ccc3OC)c2Cl)C1 10.1021/acs.jmedchem.4c01763
CHEMBL6143005 466340 0 None -4 3 Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 432 7 1 3 5.0 CCCN1CC(NC(=O)[C@@H]2C[C@H]2c2cccc(-c3cc(Cl)ccc3OC)c2Cl)C1 10.1021/acs.jmedchem.4c01763
168274920 373357 0 None -66 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 373357 0 None -66 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL3601431 487209 0 None -3 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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
172446133 387855 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
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
172457809 387855 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
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 387855 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
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 387855 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
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 278801 0 None 4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 278801 0 None 4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL503229 489006 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1593 48 23 18 -2.5 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 371922 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577523 371922 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 371922 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508068 371922 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL443071 488858 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1609 48 21 20 -2.9 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 486807 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 479291 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1864 23 22 21 -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](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 1486 31 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1025 17 13 11 -0.6 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
127036484 5482 39 None -40 7 Human 8.6 pEC50 = 8.6 Functional
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
1323 5482 39 None -40 7 Human 8.6 pEC50 = 8.6 Functional
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
92432 5482 39 None -40 7 Human 8.6 pEC50 = 8.6 Functional
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL3735690 5482 39 None -40 7 Human 8.6 pEC50 = 8.6 Functional
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL430239 5482 39 None -40 7 Human 8.6 pEC50 = 8.6 Functional
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
168278271 374186 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 374186 0 None -5 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL214332 485136 29 None -3 8 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 315941 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 315941 0 None 2 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL266417 484238 0 None -77 5 Human 8.6 pEC50 = 8.6 Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptorEvaluated for agonist activity at cloned Melanocortin 3 receptor
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)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 315289 0 None -13 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 315289 0 None -13 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
118735102 237590 0 None -8 3 Human 5.7 pEC50 = 5.7 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 237590 0 None -8 3 Human 5.7 pEC50 = 5.7 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
10257242 38928 0 None -56 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 38928 0 None -56 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
9808720 136553 0 None -48 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
9960253 136553 0 None -48 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL180892 136553 0 None -48 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 136553 0 None -48 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP releaseAgonistic potency towards human Melanocortin 3 receptor (MC3R) was determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44409240 156110 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 156110 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44415972 161345 0 None -141 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 161345 0 None -141 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
44415956 279139 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 279139 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44409240 156110 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 156110 0 None -457 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
44413832 159643 0 None -38 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210009 159643 0 None -38 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
11845444 161527 0 None -11 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 161527 0 None -11 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413969 161687 0 None -44 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 161687 0 None -44 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44413970 270536 0 None -50 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 270536 0 None -50 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44415956 279139 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 279139 0 None -24 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44394785 252087 0 None -4 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363061 252087 0 None -4 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 865 22 9 7 3.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137631599 312447 0 None -50 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 312447 0 None -50 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11845276 161513 0 None -7 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 161513 0 None -7 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
44394695 241714 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361253 241714 0 None -2 3 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 833 22 9 6 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL427629 488478 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 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
137641157 312974 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137655905 312974 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 312974 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 312974 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44413828 270545 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 270545 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
25132864 337116 0 None -42 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 337116 0 None -42 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
137634090 312222 0 None -15 5 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 312222 0 None -15 5 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL5081077 478899 0 None -29 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1983 30 28 23 -3.8 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 198143 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 198143 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cellsAgonist activity at human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44441684 194544 0 None -22 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 194544 0 None -22 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
44323015 220935 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 220935 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11845272 161812 0 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 161812 0 None -23 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44394626 138078 0 None -14 3 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183476 138078 0 None -14 3 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
25132524 350718 0 None -7 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 350718 0 None -7 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
122184637 241009 0 None -104 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 241009 0 None -104 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL409636 488073 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1604 35 21 18 -2.5 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 254200 0 None -21 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 254200 0 None -21 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration against human melanocortin 3 receptor in cAMP release assayEffective concentration against human melanocortin 3 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2370963 485646 0 None -85 2 Human 5.6 pEC50 = 5.6 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1562 47 20 18 -2.4 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 194545 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL249322 194545 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 585 7 3 5 3.5 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
118735101 237589 0 None -8128 3 Human 5.6 pEC50 = 5.6 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 237589 0 None -8128 3 Human 5.6 pEC50 = 5.6 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
168295131 375277 0 None -81 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 375277 0 None -81 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11845440 276030 0 None -23 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL377778 276030 0 None -23 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL50056 484368 1 None -15 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm060384p
10864861 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10886436 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10952071 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL140108 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL334457 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL342954 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10864861 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10864861 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None -1698 9 Human 5.6 pEC50 = 5.6 Functional
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC3R) receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
44448660 195354 0 None -281 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 195354 0 None -281 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44569175 372002 0 None -12 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 372002 0 None -12 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
127036484 5482 39 None -40 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
1323 5482 39 None -40 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
92432 5482 39 None -40 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
CHEMBL3735690 5482 39 None -40 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
CHEMBL430239 5482 39 None -40 7 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/s0960-894x(03)00114-8
CHEMBL410795 488139 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 38958 0 None -85 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 38958 0 None -85 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL524861 489128 0 None -120 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1041 16 15 11 -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](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
145990599 331665 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 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 331665 0 None -25 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 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 331500 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4282109 331500 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
11846669 161733 0 None -18 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 161733 0 None -18 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
44441644 310857 0 None -67 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 310857 0 None -67 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL434357 488601 0 None -19 3 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 795 21 8 8 2.2 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 159529 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 159529 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
137659790 315167 0 None -11 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 315167 0 None -11 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137653925 314477 0 None -64 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 314477 0 None -64 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL427205 488473 0 None 6 3 Human 7.6 pEC50 = 7.6 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 829 13 10 8 0.0 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 333565 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 333565 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2115441 485126 0 None -281 4 Human 7.6 pEC50 = 7.6 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1095 17 14 12 -1.7 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 350685 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 350685 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
145971673 329623 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217191 329623 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 837 11 12 9 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44323032 473558 0 None -14 3 Human 7.6 pEC50 = 7.6 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 473558 0 None -14 3 Human 7.6 pEC50 = 7.6 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162672255 366249 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 366249 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL383250 487626 0 None None None Human 5.6 pEC50 = 5.6 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 909 15 11 9 0.4 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 315167 0 None -11 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 315167 0 None -11 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44413829 159644 0 None -10 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 159644 0 None -10 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44445082 310359 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 310359 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
162672255 366249 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 366249 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
137656521 315577 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 315577 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44391927 28233 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 28233 0 None -100 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
168296647 375502 0 None -158 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 375502 0 None -158 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44441648 310723 0 None -18 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 310723 0 None -18 3 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44413842 270510 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 270510 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44394624 197339 0 None -60 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL266665 197339 0 None -60 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 964 27 11 9 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL410404 488116 0 None -25 5 Rat 8.5 pEC50 = 8.5 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1095 18 14 14 -1.8 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
127036484 5482 39 None -40 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
1323 5482 39 None -40 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
92432 5482 39 None -40 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL3735690 5482 39 None -40 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL430239 5482 39 None -40 7 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
145966716 329252 0 None 14 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 329252 0 None 14 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL5094168 479635 0 None -42 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1994 29 24 22 -0.7 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
CHEMBL437050 484343 3 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1570 47 21 19 -2.9 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/jm030119t
133053557 328674 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 328674 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
137633806 312402 0 None -10 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 312402 0 None -10 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL380638 487587 0 None None None Human 6.5 pEC50 = 6.5 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 843 15 10 8 0.6 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 373092 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 373092 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL413439 488283 0 None -100 3 Human 6.5 pEC50 = 6.5 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1602 47 21 18 -1.3 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 216756 0 None -42 3 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316038 216756 0 None -42 3 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394659 139242 0 None -288 3 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL186687 139242 0 None -288 3 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885712 22387 0 None -169 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 22387 0 None -169 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL185869 484955 0 None -89 3 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 19 8 7 2.0 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 314192 0 None -416 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 314192 0 None -416 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL411378 488171 0 None -56 5 Rat 7.5 pEC50 = 7.5 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1109 18 14 14 -1.5 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
172456996 388642 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
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
172468229 388642 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
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 388642 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
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 388642 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
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 276278 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 276278 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44394691 241470 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL360598 241470 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145988867 331902 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4289983 331902 0 None -12 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44413831 159642 0 None -6 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL210008 159642 0 None -6 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
172447505 388250 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
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 388250 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
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
178312196 466719 0 None 1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 533 9 1 6 3.9 COCCNC(=O)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cn(C)cn1)C1CCCN(c2cccc(C)c2)C1 10.1021/acs.jmedchem.4c01763
CHEMBL6152956 466719 0 None 1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 533 9 1 6 3.9 COCCNC(=O)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cn(C)cn1)C1CCCN(c2cccc(C)c2)C1 10.1021/acs.jmedchem.4c01763
122184910 241128 0 None -407 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 241128 0 None -407 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 328799 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 328799 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None -40 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
1323 5482 39 None -40 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
92432 5482 39 None -40 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
CHEMBL3735690 5482 39 None -40 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
CHEMBL430239 5482 39 None -40 7 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.7b00353
44577519 371951 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
44577520 371951 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL505536 371951 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 371951 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
178298635 466221 0 None -1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 454 6 2 5 5.0 O=C1NCCOc2ccc(CNCC3(c4ccc(C=C5CCSCC5)s4)CCC3)cc21 10.1021/acs.jmedchem.4c01763
CHEMBL6133378 466221 0 None -1 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 454 6 2 5 5.0 O=C1NCCOc2ccc(CNCC3(c4ccc(C=C5CCSCC5)s4)CCC3)cc21 10.1021/acs.jmedchem.4c01763
178322595 467156 0 None -4 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 453 8 2 5 4.6 CCc1ccc(-c2cc(CNC3CCN(c4ccccc4C(N)=O)C3)c(OC)cc2F)s1 10.1021/acs.jmedchem.4c01763
CHEMBL6170004 467156 0 None -4 3 Human 4.5 pEC50 = 4.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 453 8 2 5 4.6 CCc1ccc(-c2cc(CNC3CCN(c4ccccc4C(N)=O)C3)c(OC)cc2F)s1 10.1021/acs.jmedchem.4c01763
44394783 254346 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365044 254346 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 847 23 9 6 4.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
172441600 387613 0 None -77 4 Human 7.5 pEC50 = 7.5 Functional
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 387613 0 None -77 4 Human 7.5 pEC50 = 7.5 Functional
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 276248 0 None -112 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 276248 0 None -112 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL3349030 486807 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 489403 0 None -11 3 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 643 17 9 7 -0.8 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 22707 5 None -173 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 22707 5 None -173 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL410168 488101 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1527 30 20 19 -3.3 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 22122 0 None -512 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
CHEMBL1089461 22122 0 None -512 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 493 4 1 6 3.4 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1 10.1021/jm9017866
46885711 22386 0 None -123 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 22386 0 None -123 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL446185 488874 0 None 53 2 Human 7.4 pEC50 = 7.4 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 867 14 11 9 -0.6 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 276552 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 276552 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44408287 157053 0 None -288 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 157053 0 None -288 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL2371962 485793 0 None -1000 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC3R expressed in CHO cells assessed as cAMP accumulation
ChEMBL 1055 14 10 10 2.3 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]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0614275
178300807 466192 0 None -2 3 Human 4.4 pEC50 = 4.4 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 480 9 1 5 4.7 COc1ccc(C(CN(C)C)NC(=O)COc2ccc(-c3cccc4c3OCC4)cc2Cl)cc1 10.1021/acs.jmedchem.4c01763
CHEMBL6132827 466192 0 None -2 3 Human 4.4 pEC50 = 4.4 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 480 9 1 5 4.7 COc1ccc(C(CN(C)C)NC(=O)COc2ccc(-c3cccc4c3OCC4)cc2Cl)cc1 10.1021/acs.jmedchem.4c01763
11845804 161039 0 None -467 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL211419 161039 0 None -467 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5094215 479637 0 None -46 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1825 23 21 21 -0.3 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](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 374731 0 None -234 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 374731 0 None -234 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL263878 486112 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 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 374945 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 374945 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
172441036 387559 0 None -79 3 Human 7.4 pEC50 = 7.4 Functional
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 387559 0 None -79 3 Human 7.4 pEC50 = 7.4 Functional
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 477477 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 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](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 489409 0 None -35 3 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 817 20 10 8 1.1 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 241127 0 None -25 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 241127 0 None -25 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL5077811 478706 0 None -72 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1073 16 14 13 -1.6 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 478873 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1811 21 23 21 -2.2 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 328725 0 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 328725 0 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
122194229 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
1324 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
16197727 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
4836 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL3629347 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL441738 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
DB04931 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
122194229 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
1324 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
16197727 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
4836 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL3629347 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL441738 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
DB04931 621 23 None -9 9 Human 8.4 pEC50 = 8.4 Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL439128 488768 0 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1640 35 21 20 -2.6 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 278755 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL384720 278755 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
10033237 141334 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44322896 141334 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL1923662 141334 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 141334 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25133210 334033 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 334033 0 None -44 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
44322787 215649 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 215649 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162669632 356382 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 356382 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL409049 488045 0 None None None Human 6.4 pEC50 = 6.4 Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
ChEMBL 1555 30 20 19 -2.5 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 313181 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL407680 313181 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1443 31 14 21 -1.9 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
16007263 161259 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 161259 0 None -23 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44394784 254268 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365019 254268 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 861 23 9 7 3.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885526 22083 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
CHEMBL1089135 22083 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 456 4 1 5 3.2 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1 10.1021/jm9017866
44413931 159593 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 159593 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
101043845 332258 1 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
145948876 332258 1 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 332258 1 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5177536 332258 1 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL3349030 486807 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 196934 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263234 196934 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL382369 487619 0 None None None Human 5.4 pEC50 = 5.4 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 859 15 11 9 -0.8 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 310722 0 None -89 3 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399714 310722 0 None -89 3 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 631 8 2 7 4.1 Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
168278924 374139 0 None -67 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 374139 0 None -67 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
44569176 337063 0 None -48 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 337063 0 None -48 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
25129107 347856 0 None -36 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 347856 0 None -36 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL184870 484953 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 770 20 10 6 1.9 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 312000 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 312000 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44408154 278594 0 None -77 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 278594 0 None -77 4 Human 6.4 pEC50 = 6.4 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
44322788 313283 0 None -58 3 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 313283 0 None -58 3 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394690 252670 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL364119 252670 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168285101 374705 0 None -213 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 374705 0 None -213 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
46885760 22594 0 None -102 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
CHEMBL1092550 22594 0 None -102 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F 10.1021/jm9017866
44394582 333072 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434544 333072 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL3600840 487199 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 312974 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137655905 312974 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 312974 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 312974 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44394581 240730 0 None -12 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359702 240730 0 None -12 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46885482 22645 0 None -81 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092860 22645 0 None -81 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44394580 240729 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359701 240729 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145972289 329453 0 None 21 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 329453 0 None 21 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
127036484 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
1323 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
92432 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
CHEMBL3735690 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
CHEMBL430239 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
137637283 311907 0 None -15 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 311907 0 None -15 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC3R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
127036484 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
1323 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
92432 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL3735690 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL430239 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
127036484 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
1323 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
92432 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL3735690 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL430239 5482 39 None -40 7 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
172445559 387810 0 None -5 4 Human 8.3 pEC50 = 8.3 Functional
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 387810 0 None -5 4 Human 8.3 pEC50 = 8.3 Functional
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 487882 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1145 18 14 14 -0.7 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 485877 0 None -53 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 1024 17 13 12 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)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 161825 0 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 161825 0 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL437050 484343 3 None 2 4 Human 8.2 pEC50 = 8.2 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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
44577514 336975 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577515 336975 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 336975 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 336975 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
172468014 388892 0 None -31 3 Human 7.3 pEC50 = 7.3 Functional
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 388892 0 None -31 3 Human 7.3 pEC50 = 7.3 Functional
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 22595 0 None -15 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092571 22595 0 None -15 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
178304576 466973 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 540 8 1 4 4.8 O=C(NCC(F)F)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cc2c(cn1)CCCC2)[C@H]1C[C@@H](N2CCCC2)C1 10.1021/acs.jmedchem.4c01763
CHEMBL6165558 466973 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 540 8 1 4 4.8 O=C(NCC(F)F)C(C1CC2(C1)CC21CCC1)N(C(=O)c1cc2c(cn1)CCCC2)[C@H]1C[C@@H](N2CCCC2)C1 10.1021/acs.jmedchem.4c01763
168277543 373759 0 None -125 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 373759 0 None -125 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAgonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44577510 371922 0 None -2 4 Human 5.3 pEC50 = 5.3 Functional
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
44577523 371922 0 None -2 4 Human 5.3 pEC50 = 5.3 Functional
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 371922 0 None -2 4 Human 5.3 pEC50 = 5.3 Functional
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
CHEMBL508068 371922 0 None -2 4 Human 5.3 pEC50 = 5.3 Functional
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 371891 0 None -30 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 371891 0 None -30 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
122184911 241129 0 None -89 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 241129 0 None -89 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
118735099 237587 0 None -173 2 Human 7.3 pEC50 = 7.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 237587 0 None -173 2 Human 7.3 pEC50 = 7.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
25133209 347449 0 None -19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 347449 0 None -19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL437050 484343 3 None 2 4 Human 6.3 pEC50 = 6.3 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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
137636965 312140 0 None -13 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 312140 0 None -13 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44408173 157068 0 None -102 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 157068 0 None -102 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44413876 161208 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 161208 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 161208 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 161208 0 None -93 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
25132526 372096 0 None -69 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
CHEMBL507876 372096 0 None -69 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
118735103 237591 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 237591 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44408253 277631 0 None -38 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 277631 0 None -38 4 Human 6.3 pEC50 = 6.3 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL183315 484945 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 729 18 8 6 1.3 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 136874 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181494 136874 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44577519 371951 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 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
44577520 371951 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 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 371951 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 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 371951 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 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 478768 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1853 23 23 21 -1.1 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 276031 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 276031 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
145988152 331848 0 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 331848 0 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
46885759 22592 0 None -95 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092548 22592 0 None -95 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
44322994 216651 0 None -60 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315258 216651 0 None -60 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25129108 346831 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL450236 346831 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
44322977 221066 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 221066 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11061068 64921 0 None -58 3 Human 7.2 pEC50 = 7.2 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
44441641 64921 0 None -58 3 Human 7.2 pEC50 = 7.2 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 64921 0 None -58 3 Human 7.2 pEC50 = 7.2 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL250508 64921 0 None -58 3 Human 7.2 pEC50 = 7.2 Functional
Evaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at MC3R as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL2372365 485840 0 None -1 3 Rat 7.2 pEC50 = 7.2 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1081 17 13 14 -0.3 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 277834 0 None -104 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 277834 0 None -104 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44413932 274948 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 274948 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
44415918 278765 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 278765 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44275650 194469 0 None -15 4 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 194469 0 None -15 4 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
44322895 328350 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 328350 0 None -3 3 Human 8.2 pEC50 = 8.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370964 485647 0 None -99 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 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 485647 0 None -99 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assayAgonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as increase in cAMP level by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 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 478889 0 None -9 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1887 23 23 21 -0.9 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 479421 0 None -8 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1862 25 26 22 -3.1 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
CHEMBL214332 485136 29 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 485136 29 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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
122194229 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
1324 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
16197727 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
4836 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
CHEMBL3629347 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
CHEMBL441738 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
DB04931 621 23 None -9 9 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/acs.jmedchem.7b00353
162670951 366217 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 366217 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
46885558 22128 0 None -151 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089483 22128 0 None -151 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
162670951 366217 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 366217 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL509582 489086 0 None -3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL 1072 14 13 11 -0.2 CCCC[C@H](NC(C)=O)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 388312 0 None -467 4 Human 7.2 pEC50 = 7.2 Functional
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 388312 0 None -467 4 Human 7.2 pEC50 = 7.2 Functional
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 312162 0 None -69 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 312162 0 None -69 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL411400 488173 0 None -457 5 Rat 7.2 pEC50 = 7.2 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1123 18 14 14 -1.0 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 157086 0 None -75 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 157086 0 None -75 4 Human 6.2 pEC50 = 6.2 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44323034 473488 0 None -46 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 473488 0 None -46 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44394735 251395 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361578 251395 0 None -34 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
168273822 373658 0 None -162 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 373658 0 None -162 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
46885481 22074 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089104 22074 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL415200 488390 0 None -77 5 Rat 6.2 pEC50 = 6.2 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1053 17 12 14 -1.2 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 484952 0 None -16 3 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 765 19 8 7 0.8 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 251396 0 None -25 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361579 251396 0 None -25 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11846844 270569 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 270569 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44441642 310455 0 None -53 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 310455 0 None -53 3 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137640703 313008 0 None -1202 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 313008 0 None -1202 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL264190 484234 0 None -1 7 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 685 18 10 7 -0.4 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 484234 0 None -1 7 Human 8.2 pEC50 = 8.2 Functional
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 685 18 10 7 -0.4 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 487926 0 None -66 5 Rat 8.1 pEC50 = 8.1 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1129 18 14 14 -1.1 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 478670 0 None -57 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1938 27 26 22 -1.9 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](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 388642 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
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
172468229 388642 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
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 388642 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
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 388642 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
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
CHEMBL437050 484343 3 None 2 4 Human 6.2 pEC50 = 6.2 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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
10146211 136659 0 None -11748 3 Human 5.2 pEC50 = 5.2 Functional
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 136659 0 None -11748 3 Human 5.2 pEC50 = 5.2 Functional
Effective concentration determined against melanocortin-3 receptorEffective concentration determined against melanocortin-3 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
122184577 241003 0 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 241003 0 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
46885480 22073 0 None -4 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 22073 0 None -4 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44322812 221867 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 221867 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075506 478577 0 None -512 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1925 26 23 22 -0.9 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 313740 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4083755 313740 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1122 22 14 16 -1.6 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
145964837 329293 0 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 329293 0 None -10 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
137646617 313441 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 313441 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46885524 22123 0 None -354 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1089462 22123 0 None -354 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL406891 487928 0 None -34 5 Rat 7.1 pEC50 = 7.1 Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)Maximal agonist response at rat melanocortin 3 receptor (MC3R)
ChEMBL 1109 18 14 14 -1.4 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 486807 0 None 1 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 487207 0 None -12 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 260355 0 None -53 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL369770 260355 0 None -53 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137647538 313847 0 None -1445 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 313847 0 None -1445 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
145975465 328911 0 None -11 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 328911 0 None -11 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145964017 328999 0 None -23 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 328999 0 None -23 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
46919520 39036 0 None -691 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 39036 0 None -691 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 3 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
162643435 355513 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 355513 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 355513 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 355513 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
122184912 241131 0 None -2 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 241131 0 None -2 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
49862377 38939 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 38939 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL3600921 487206 0 None 1 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 313647 0 None -38 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4082585 313647 0 None -38 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1127 22 14 17 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
11845438 275020 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL375775 275020 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44394627 252126 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363272 252126 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44416135 161642 0 None -38 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 161642 0 None -38 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3RAgonist activity at human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
25133208 336521 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 336521 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
44441646 310159 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 310159 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human MC3R assessed as stimulation of cAMP productionAntagonist activity at human MC3R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL88185 489400 0 None -38 3 Human 6.1 pEC50 = 6.1 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 721 19 9 8 -1.2 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 347061 0 None -18 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
CHEMBL451694 347061 0 None -18 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
44413930 270519 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 270519 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44394787 330849 0 None -4 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL425348 330849 0 None -4 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181161 484884 0 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 744 18 9 6 1.1 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 139053 0 None -63 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL185868 139053 0 None -63 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137636677 312024 0 None -295 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 312024 0 None -295 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11845813 277109 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 277109 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3R transfected in HEK293 cellsAgonist activity at human MC3R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL410217 488105 0 None -30 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptorEffective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor
ChEMBL 981 12 13 11 -2.4 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 277946 0 None -54 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 277946 0 None -54 4 Human 6.1 pEC50 = 6.1 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862378 38940 0 None -52 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 38940 0 None -52 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
44394584 196906 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263047 196906 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44323029 474096 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 474096 0 None -1 3 Human 8.0 pEC50 = 8.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285801 374542 0 None 13 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 374542 0 None 13 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600841 487200 0 None 26 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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 38937 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 38937 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC3 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
178297566 466670 0 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 400 5 1 3 4.8 Cc1ccc(-c2cc(Cl)cs2)cc1C1(C(=O)NC2CN(C3CCC3)C2)CC1 10.1021/acs.jmedchem.4c01763
CHEMBL6151620 466670 0 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 400 5 1 3 4.8 Cc1ccc(-c2cc(Cl)cs2)cc1C1(C(=O)NC2CN(C3CCC3)C2)CC1 10.1021/acs.jmedchem.4c01763
163196518 375167 5 None -301 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 375167 5 None -301 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
172461542 389138 0 None -331 3 Human 7.0 pEC50 = 7.0 Functional
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 389138 0 None -331 3 Human 7.0 pEC50 = 7.0 Functional
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 484957 0 None -30 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 753 19 9 7 3.1 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 195446 0 None -89 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 195446 0 None -89 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL359765 487190 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 806 19 10 6 3.2 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 197060 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 197060 0 None -20 3 Human 7.0 pEC50 = 7.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
178311805 466199 0 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 402 3 1 3 4.6 CC1CC(N2CCCC2)CN1C(=O)c1cc(O)cc(-c2cc(Cl)ccc2F)c1 10.1021/acs.jmedchem.4c01763
CHEMBL6133006 466199 0 None None None Human 4.0 pEC50 = 4.0 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysisAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of ACTH-induced cAMP accumulation measured after 70 mins incubation by fluorescence analysis
ChEMBL 402 3 1 3 4.6 CC1CC(N2CCCC2)CN1C(=O)c1cc(O)cc(-c2cc(Cl)ccc2F)c1 10.1021/acs.jmedchem.4c01763
24774356 195215 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253574 195215 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 861 9 10 8 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL5091245 479465 0 None -26 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1911 26 24 22 -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](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 488367 0 None -630 4 Human 6.0 pEC50 = 6.0 Functional
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
ChEMBL 1578 47 20 20 -2.5 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 254748 0 None -13 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365385 254748 0 None -13 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 759 20 8 7 1.0 COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448629 327664 0 None -194 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 327664 0 None -194 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MC3R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC3R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2112008 485087 0 None 5 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptorEffective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor
ChEMBL 1570 47 21 19 -2.9 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 216794 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 216794 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132867 337017 0 None -38 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 337017 0 None -38 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC3R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44408276 157173 0 None -162 4 Human 6.0 pEC50 = 6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 157173 0 None -162 4 Human 6.0 pEC50 = 6 Functional
Activity against human MC3R by cAMP accumulationActivity against human MC3R by cAMP accumulation
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44391999 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None -70 4 Human 6.0 pEC50 = 6 Functional
Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44394692 138507 0 None -33 3 Human 6.0 pEC50 = 6 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184466 138507 0 None -33 3 Human 6.0 pEC50 = 6 Functional
Agonistic activity against human Melanocortin 3 receptorAgonistic activity against human Melanocortin 3 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11753695 22707 5 None -501 6 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 22707 5 None -501 6 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL2370968 485651 0 None -2 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1561 44 19 17 -1.4 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 485651 0 None -2 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1561 44 19 17 -1.4 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 485647 0 None -32 4 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 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 485647 0 None -32 4 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1601 47 21 18 -1.9 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
177639611 390482 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1224 18 14 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)Cc3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5542612 390482 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1224 18 14 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)Cc3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177639611 390482 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1224 18 14 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)Cc3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5542612 390482 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1224 18 14 12 0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)Cc3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162643518 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -46 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177653088 391358 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1233 20 19 13 -2.5 CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
CHEMBL5567528 391358 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1233 20 19 13 -2.5 CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
177653088 391358 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1233 20 19 13 -2.5 CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
CHEMBL5567528 391358 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1233 20 19 13 -2.5 CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
162677173 366864 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 366864 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677173 366864 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799891 366864 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 18 14 11 0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177653580 391638 0 None -6 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 19 14 15 -0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCC(=O)O)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572145 391638 0 None -6 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 19 14 15 -0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCC(=O)O)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654332 391746 0 None -20 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 16 12 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)N)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.3c01822
CHEMBL5574077 391746 0 None -20 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 16 12 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)N)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.3c01822
177654332 391746 0 None -20 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 16 12 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)N)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.3c01822
CHEMBL5574077 391746 0 None -20 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 16 12 -0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)N)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.3c01822
177653580 391638 0 None -6 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 19 14 15 -0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCC(=O)O)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572145 391638 0 None -6 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 19 14 15 -0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCC(=O)O)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162664942 356020 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 356020 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177647514 392078 0 None -2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1246 22 16 12 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](CCCCNC(=N)NCCC)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.3c01822
CHEMBL5590202 392078 0 None -2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1246 22 16 12 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](CCCCNC(=N)NCCC)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.3c01822
177647514 392078 0 None -2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1246 22 16 12 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](CCCCNC(=N)NCCC)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.3c01822
CHEMBL5590202 392078 0 None -2 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1246 22 16 12 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](CCCCNC(=N)NCCC)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.3c01822
177654415 390562 0 None -4 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5550011 390562 0 None -4 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654415 390562 0 None -4 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5550011 390562 0 None -4 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177653008 390483 0 None -5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1238 18 16 12 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](Cc2ccc(NC(=N)N)cc2)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.3c01822
CHEMBL5542650 390483 0 None -5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1238 18 16 12 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](Cc2ccc(NC(=N)N)cc2)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.3c01822
177653008 390483 0 None -5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1238 18 16 12 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](Cc2ccc(NC(=N)N)cc2)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.3c01822
CHEMBL5542650 390483 0 None -5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1238 18 16 12 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](Cc2ccc(NC(=N)N)cc2)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.3c01822
177653954 391662 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1288 24 15 12 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](CCCCNC(=N)N(CCC)CCC)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.3c01822
CHEMBL5572575 391662 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1288 24 15 12 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](CCCCNC(=N)N(CCC)CCC)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.3c01822
177653954 391662 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1288 24 15 12 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](CCCCNC(=N)N(CCC)CCC)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.3c01822
CHEMBL5572575 391662 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1288 24 15 12 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](CCCCNC(=N)N(CCC)CCC)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.3c01822
177656587 391437 0 None -38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1257 20 16 15 -1.4 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5568902 391437 0 None -38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1257 20 16 15 -1.4 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656587 391437 0 None -38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1257 20 16 15 -1.4 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5568902 391437 0 None -38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1257 20 16 15 -1.4 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177653243 390463 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1294 22 16 12 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCc2ccccc2)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.3c01822
CHEMBL5542391 390463 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1294 22 16 12 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCc2ccccc2)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.3c01822
177653243 390463 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1294 22 16 12 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCc2ccccc2)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.3c01822
CHEMBL5542391 390463 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1294 22 16 12 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCc2ccccc2)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.3c01822
177649626 392066 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1247 22 17 13 -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](CCCCNC(=N)NCCN)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.3c01822
CHEMBL5589988 392066 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1247 22 17 13 -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](CCCCNC(=N)NCCN)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.3c01822
162644475 355644 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 355644 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162644475 355644 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4778074 355644 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
177649626 392066 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1247 22 17 13 -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](CCCCNC(=N)NCCN)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.3c01822
CHEMBL5589988 392066 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1247 22 17 13 -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](CCCCNC(=N)NCCN)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.3c01822
177654908 391599 0 None -4 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1210 17 14 12 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5571514 391599 0 None -4 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1210 17 14 12 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654908 391599 0 None -4 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1210 17 14 12 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5571514 391599 0 None -4 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1210 17 14 12 0.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.3c01822
101043845 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
145948876 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL4299441 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
101043845 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
145948876 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL4299441 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
CHEMBL5177536 332258 1 None 3 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC3R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 30 nM alpha-MSH by split luciferase cAMP sensor dynamic assay
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.1c01295
177655585 391720 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1162 19 14 12 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](CCCCN)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.3c01822
CHEMBL5573419 391720 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1162 19 14 12 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](CCCCN)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.3c01822
177655585 391720 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1162 19 14 12 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](CCCCN)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.3c01822
CHEMBL5573419 391720 0 None -3 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1162 19 14 12 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](CCCCN)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.3c01822
171905197 390550 0 None -5 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1190 19 16 12 -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](CCCNC(=N)N)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.3c01822
CHEMBL5549790 390550 0 None -5 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1190 19 16 12 -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](CCCNC(=N)N)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.3c01822
171905197 390550 0 None -5 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1190 19 16 12 -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](CCCNC(=N)N)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.3c01822
CHEMBL5549790 390550 0 None -5 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1190 19 16 12 -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](CCCNC(=N)N)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.3c01822
177654395 391902 0 None -4 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1234 17 13 14 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccc4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5579693 391902 0 None -4 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1234 17 13 14 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccc4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654395 391902 0 None -4 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1234 17 13 14 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccc4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5579693 391902 0 None -4 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1234 17 13 14 0.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccc4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162668987 356405 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 356405 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 356405 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 356405 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 366659 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 366659 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162674869 366659 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4797266 366659 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1114 16 14 11 0.9 CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177657335 391290 0 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5566348 391290 0 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654096 391103 0 None -2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1276 23 17 13 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCCC(=O)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.3c01822
CHEMBL5563448 391103 0 None -2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1276 23 17 13 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCCC(=O)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.3c01822
177657335 391290 0 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5566348 391290 0 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654096 391103 0 None -2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1276 23 17 13 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCCC(=O)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.3c01822
CHEMBL5563448 391103 0 None -2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1276 23 17 13 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCCNC(=N)NCCC(=O)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.3c01822
162665567 356174 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 356174 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
162665567 356174 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784635 356174 0 None -4 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1110 16 12 10 2.0 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O 10.1021/acs.jmedchem.0c01620
177656286 391586 0 None -13 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5571320 391586 0 None -13 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656286 391586 0 None -13 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5571320 391586 0 None -13 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162672763 366485 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 366485 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 366485 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 366485 0 None -6 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162667953 356354 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 356354 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
162667953 356354 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787322 356354 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1088 15 12 10 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/acs.jmedchem.0c01620
177655006 391824 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 15 12 -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](CCCNC(N)=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.3c01822
CHEMBL5575419 391824 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 15 12 -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](CCCNC(N)=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.3c01822
177655006 391824 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 15 12 -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](CCCNC(N)=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.3c01822
CHEMBL5575419 391824 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 15 12 -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](CCCNC(N)=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.3c01822
177656778 391834 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1148 18 14 12 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCN)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.3c01822
CHEMBL5575530 391834 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1148 18 14 12 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCN)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.3c01822
177656778 391834 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1148 18 14 12 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCN)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.3c01822
CHEMBL5575530 391834 0 None -4 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1148 18 14 12 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCN)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.3c01822
162675203 366609 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 366609 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675203 366609 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4796506 366609 0 None -10 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1122 16 14 11 1.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177655182 391526 0 None -25 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1201 18 14 15 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCN)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5570494 391526 0 None -25 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1201 18 14 15 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCN)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177655182 391526 0 None -25 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1201 18 14 15 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCN)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5570494 391526 0 None -25 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1201 18 14 15 -1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCN)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
10855168 355744 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 355744 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
177654085 391068 0 None -8 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5562859 391068 0 None -8 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177654085 391068 0 None -8 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5562859 391068 0 None -8 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1243 19 16 15 -1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(CCNC(=N)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
10855168 355744 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4779301 355744 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1050 15 13 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/acs.jmedchem.0c01620
162673931 366422 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 366422 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 366422 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 366422 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
101176453 366336 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 366336 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
101176453 366336 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4792986 366336 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1034 15 12 10 0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.0c01620
177652728 391245 0 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 17 13 -2.0 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
CHEMBL5565453 391245 0 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 17 13 -2.0 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
11434732 391847 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1091 15 12 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[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]2CCCN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5575814 391847 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1091 15 12 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[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]2CCCN2C1=O 10.1021/acs.jmedchem.3c01822
177660740 390763 0 None -43 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5557625 390763 0 None -43 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
11993702 484262 27 None -19 4 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assayAgonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
CHEMBL3301624 484262 27 None -19 4 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assayAgonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
DB11700 484262 27 None -19 4 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assayAgonist activity at human MC3R expressed in CHO-K1 cells incubated for 40 mins by electro-chemiluminescence assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
11434732 391847 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1091 15 12 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[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]2CCCN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5575814 391847 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1091 15 12 11 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[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]2CCCN2C1=O 10.1021/acs.jmedchem.3c01822
177660740 390763 0 None -43 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5557625 390763 0 None -43 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656185 391289 0 None -28 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 20 16 14 -1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCC(=O)O)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5566308 391289 0 None -28 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 20 16 14 -1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCC(=O)O)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656185 391289 0 None -28 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 20 16 14 -1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCC(=O)O)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5566308 391289 0 None -28 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 20 16 14 -1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCC(=O)O)CN2C1=O 10.1021/acs.jmedchem.3c01822
177652728 391245 0 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 17 13 -2.0 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
CHEMBL5565453 391245 0 None -10 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1191 19 17 13 -2.0 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)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.3c01822
162643518 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -46 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 366798 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 366798 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162675582 366798 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4799036 366798 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 16 14 11 0.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177656803 391846 0 None -7 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1240 17 13 14 1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C4CCCCC4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5575805 391846 0 None -7 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1240 17 13 14 1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C4CCCCC4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656803 391846 0 None -7 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1240 17 13 14 1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C4CCCCC4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5575805 391846 0 None -7 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1240 17 13 14 1.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C4CCCCC4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177657135 391837 0 None -6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1242 21 13 14 1.3 CCCCCCc1cn([C@H]2C[C@H]3C(=O)N[C@H](Cc4ccc5ccccc5c4)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N3C2)nn1 10.1021/acs.jmedchem.3c01822
CHEMBL5575572 391837 0 None -6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1242 21 13 14 1.3 CCCCCCc1cn([C@H]2C[C@H]3C(=O)N[C@H](Cc4ccc5ccccc5c4)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N3C2)nn1 10.1021/acs.jmedchem.3c01822
162672837 366387 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 366387 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 366387 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 366387 0 None -17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
177657135 391837 0 None -6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1242 21 13 14 1.3 CCCCCCc1cn([C@H]2C[C@H]3C(=O)N[C@H](Cc4ccc5ccccc5c4)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N3C2)nn1 10.1021/acs.jmedchem.3c01822
CHEMBL5575572 391837 0 None -6 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1242 21 13 14 1.3 CCCCCCc1cn([C@H]2C[C@H]3C(=O)N[C@H](Cc4ccc5ccccc5c4)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N3C2)nn1 10.1021/acs.jmedchem.3c01822
177652581 391670 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572691 391670 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177652581 391670 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572691 391670 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1235 17 13 15 0.3 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(-c4ccccn4)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656029 391788 0 None -87 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5574804 391788 0 None -87 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
177656029 391788 0 None -87 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5574804 391788 0 None -87 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1219 19 17 13 -2.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CCNC(=N)N)CN2C1=O 10.1021/acs.jmedchem.3c01822
177644684 392215 0 None -47 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5592759 392215 0 None -47 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177644684 392215 0 None -47 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5592759 392215 0 None -47 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1215 17 14 15 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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](n3cc(C(C)(C)N)nn3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162676295 366791 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 366791 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 366892 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 366892 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 366892 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 366892 0 None -9 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 366791 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 366791 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 355566 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 355566 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 355566 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 355566 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
127035019 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
1325 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
9898183 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
CHEMBL3422426 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
CHEMBL3735607 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
127035019 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
1325 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
9898183 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
CHEMBL3422426 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
CHEMBL3735607 7320 11 None -131 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.3c01822
177655556 391655 0 None -36 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1220 20 16 14 -2.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCCN)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572502 391655 0 None -36 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1220 20 16 14 -2.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCCN)CN2C1=O 10.1021/acs.jmedchem.3c01822
177655556 391655 0 None -36 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1220 20 16 14 -2.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCCN)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5572502 391655 0 None -36 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1220 20 16 14 -2.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)[C@@H](N)CCCN)CN2C1=O 10.1021/acs.jmedchem.3c01822
162673650 366417 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 366417 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 366417 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 366417 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
127035019 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
1325 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
9898183 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3735607 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
127035019 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
1325 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
9898183 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3735607 7320 11 None -131 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
177647940 391957 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 14 12 0.4 CCCCCC(=O)N[C@H]1C[C@H]2C(=O)N[C@H](Cc3ccc4ccccc4c3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N2C1 10.1021/acs.jmedchem.3c01822
CHEMBL5583794 391957 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 14 12 0.4 CCCCCC(=O)N[C@H]1C[C@H]2C(=O)N[C@H](Cc3ccc4ccccc4c3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N2C1 10.1021/acs.jmedchem.3c01822
177647940 391957 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 14 12 0.4 CCCCCC(=O)N[C@H]1C[C@H]2C(=O)N[C@H](Cc3ccc4ccccc4c3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N2C1 10.1021/acs.jmedchem.3c01822
CHEMBL5583794 391957 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1204 20 14 12 0.4 CCCCCC(=O)N[C@H]1C[C@H]2C(=O)N[C@H](Cc3ccc4ccccc4c3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@H](C(N)=O)CCCCNC(=O)C[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N2C1 10.1021/acs.jmedchem.3c01822
177653150 391557 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 18 14 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CC3CCCCC3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5570854 391557 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 18 14 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CC3CCCCC3)CN2C1=O 10.1021/acs.jmedchem.3c01822
177653150 391557 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 18 14 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CC3CCCCC3)CN2C1=O 10.1021/acs.jmedchem.3c01822
CHEMBL5570854 391557 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assayAntagonist activity at C-terminal HA-tagged human MC3-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL 1230 18 14 12 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)CNC(=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(=O)CC3CCCCC3)CN2C1=O 10.1021/acs.jmedchem.3c01822
162664942 356020 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4782808 356020 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1158 16 14 11 1.3 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL253364 486024 0 None None None Human 10.6 pKd = 10.6 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 932 11 13 10 -0.3 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 310362 0 None None None Human 9.8 pKd = 9.8 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 310362 0 None None None Human 9.8 pKd = 9.8 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
122184576 241002 0 None None None Human 9.1 pKd = 9.1 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 241002 0 None None None Human 9.1 pKd = 9.1 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL2096742 484199 0 None None None Human 8.7 pKd = 8.7 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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 241007 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None None None Human 8.0 pKd = 8 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184633 241005 0 None None None Human 8.5 pKd = 8.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 241005 0 None None None Human 8.5 pKd = 8.5 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413573 488288 0 None None None Human 8.4 pKd = 8.4 Functional
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL 879 13 10 8 1.2 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 197396 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 197396 0 None None None Human 8.3 pKd = 8.3 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL266417 484238 0 None None None Human 8.3 pKd = 8.3 Functional
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptor
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)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 488525 0 None None None Human 8.3 pKd = 8.3 Functional
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 3 receptor
ChEMBL 1149 17 13 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](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL3600912 487203 0 None None None Human 8.2 pKd = 8.2 Functional
Antagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC3 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 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)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
122194229 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
1324 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
16197727 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
4836 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL3629347 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL441738 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
DB04931 621 23 None -165 9 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
10408 1486 31 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central 1025 17 13 11 -0.6 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 1486 31 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
Drug Central 1025 17 13 11 -0.6 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 6262 0 None None None Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17482720
1334 3090 0 None None None Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11150170
1341 6264 0 None -6 3 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12431055
1329 645 0 None None None Mouse 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
Q03288 645 0 None None None Mouse 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9454589
1335 647 0 None -39 3 Human 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9819197
O00253 647 0 None -39 3 Human 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9819197


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1971 5840 38 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5840 38 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5840 38 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5840 38 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5840 38 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 221077 40 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 221077 40 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB06202 221077 40 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 234502 70 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 234502 70 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB09330 234502 70 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2579 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
5362436 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01079 8225 26 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8400 48 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 7298 64 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 7298 64 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 7298 64 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 7298 64 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 7298 64 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
25025298 159796 46 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
25181577 159796 46 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 159796 46 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB12095 159796 46 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
176 823 54 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 823 54 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 823 54 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 823 54 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 823 54 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 18649 37 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 18649 37 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01244 18649 37 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 466276 75 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 466276 75 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00339 466276 75 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1933 51 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1933 51 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1933 51 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1933 51 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1933 51 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
1821 410750 60 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
4212 410750 60 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 410750 60 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01204 410750 60 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00507 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 352530 47 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 352530 47 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB06401 352530 47 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6773 56 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6773 56 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6773 56 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6773 56 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6773 56 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 25079 69 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 25079 69 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB08901 25079 69 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
183 84935 67 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2162 84935 67 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 84935 67 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00381 84935 67 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 474146 33 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 474146 33 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB13766 474146 33 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 23729 35 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 23729 35 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01177 23729 35 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38402 12 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38402 12 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38402 12 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38402 12 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB06816 38402 12 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2630 62383 30 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 62383 30 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 62383 30 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 62383 30 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 125802 64 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 125802 64 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB13853 125802 64 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB06616 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3415 38 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3415 38 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3415 38 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3415 38 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3415 38 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 46619 13 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 46619 13 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01544 46619 13 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 4113 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 4113 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 4113 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 4113 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 4113 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5045 22 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
1634 163834 36 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
4011 163834 36 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 163834 36 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00934 163834 36 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1895 54 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1895 54 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1895 54 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1895 54 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1895 54 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1608 53 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1608 53 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1608 53 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1608 53 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1608 53 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 450637 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 450637 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB08865 450637 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
623 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
667466 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1897 43 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6857 72 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6857 72 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6857 72 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6857 72 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6857 72 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 44053 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
224 44053 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 44053 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 44053 46 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 23462 27 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 23462 27 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB13384 23462 27 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 120201 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 120201 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB13434 120201 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
1826 57626 32 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
4236 57626 32 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 57626 32 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00745 57626 32 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8980 49 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8980 49 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8980 49 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8980 49 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8980 49 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3105 49 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3105 49 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3105 49 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3105 49 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3105 49 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
180 829 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
200 829 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 829 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 829 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 829 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 2860 75 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 2860 75 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 2860 75 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 2860 75 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 2860 75 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470126 66 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470126 66 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00281 470126 66 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 47615 74 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2459 47615 74 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 47615 74 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00398 47615 74 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1042 63 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1042 63 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1042 63 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1042 63 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1042 63 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
CHEMBL6066864 479735 0 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
3149 26881 13 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 26881 13 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB11594 26881 13 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3909 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3909 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3909 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3909 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3909 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
9852188 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
CHEMBL3833333 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB14011 1630 28 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
3155 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
951 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 77368 13 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8655 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8655 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8655 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8655 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8655 40 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 474294 78 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 474294 78 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00317 474294 78 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2818 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
CHEMBL253391 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1973 61 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38344 24 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 38344 24 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 159957 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 159957 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB11963 159957 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 202914 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
977 202914 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 202914 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 202914 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
1868 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
25077405 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
3902 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
49800011 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
CHEMBL1201309 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
DB00666 5535 0 None None None Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1322 33 16 15 -1.6 CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](Cc1cc2ccccc2cc1)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 10.1038/s41467-023-40064-9
2398 1965 48 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1965 48 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1965 48 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1965 48 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1965 48 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 25278 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 25278 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB08916 25278 68 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1662 62 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1662 62 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1662 62 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1662 62 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 1662 62 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 125224 40 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 125224 40 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00694 125224 40 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6468 43 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6468 43 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6468 43 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6468 43 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6468 43 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 117955 32 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 117955 32 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01220 117955 32 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB00878 470127 64 None None None Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 78550 5 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 78550 5 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB13500 78550 5 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6124 31 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
4329 6124 31 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9941444 6124 31 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL3349607 6124 31 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB06663 6124 31 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human MC3R in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H]2N(C(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccc(cc1)OCc1ccccc1)Cc1ccccc1)C[C@@H](C2)OC(=O)NCCN)c1ccccc1)Cc1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2600 8239 59 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8239 59 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8239 59 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8239 59 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8239 59 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3407 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3407 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3407 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3407 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3407 55 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3419 44 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3419 44 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3419 44 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3419 44 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3419 44 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 26122 15 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
3018 26122 15 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 26122 15 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB11125 26122 15 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 387203 55 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 387203 55 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01268 387203 55 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2436 470362 35 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
68617 470362 35 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 470362 35 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01104 470362 35 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8173 46 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8173 46 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8173 46 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8173 46 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8173 46 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
2106 461821 25 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
4746 461821 25 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 461821 25 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
DB01074 461821 25 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
1887 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 5630 45 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6358 55 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6358 55 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6358 55 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6358 55 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6358 55 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8289 46 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8289 46 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8289 46 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8289 46 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 8289 46 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6448 36 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6448 36 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6448 36 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6448 36 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 6448 36 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3351 39 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3351 39 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3351 39 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3351 39 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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 3351 39 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human MC3R in an in vitro assay with cellular 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
122194229 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
1324 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
16197727 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
4836 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
CHEMBL3629347 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
CHEMBL441738 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
DB04931 621 23 None None None Human 9.9 pEC50 = 9.9 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm0303103
127036484 5482 39 None None None Human 9.6 pEC50 = 9.6 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0303103
1323 5482 39 None None None Human 9.6 pEC50 = 9.6 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0303103
92432 5482 39 None None None Human 9.6 pEC50 = 9.6 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0303103
CHEMBL3735690 5482 39 None None None Human 9.6 pEC50 = 9.6 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0303103
CHEMBL430239 5482 39 None None None Human 9.6 pEC50 = 9.6 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0303103
CHEMBL214332 485136 29 None None None Human 9.2 pEC50 = 9.2 Binding
Effective concentration required for the biological activity against human Melanocortin 3 receptorEffective concentration required for the biological activity against human Melanocortin 3 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 477645 0 None None None Human 8.7 pEC50 = 8.7 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 1038 17 14 11 -0.6 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 216671 0 None None None Human 6.0 pEC50 = 6 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL315397 216671 0 None None None Human 6.0 pEC50 = 6 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44323233 216377 0 None None None Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 216377 0 None None None Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL188738 484961 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 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 484968 0 None None None Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 10 10 -1.2 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 79296 0 None None None Human 5.8 pEC50 = 5.8 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
11763303 79296 0 None None None Human 5.8 pEC50 = 5.8 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL14416 79296 0 None None None Human 5.8 pEC50 = 5.8 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL446941 79296 0 None None None Human 5.8 pEC50 = 5.8 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 545 12 3 6 2.9 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2c[nH]cn2)CC1 10.1021/jm025600i
44323020 333622 0 None None None Human 7.8 pEC50 = 7.8 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 333622 0 None None None Human 7.8 pEC50 = 7.8 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL188459 484959 0 None None None Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 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 487489 0 None None None Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 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 198615 0 None None None Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL275067 198615 0 None None None Human 5.7 pEC50 = 5.7 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 587 13 3 6 3.1 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1 10.1021/jm025600i
CHEMBL373344 487492 0 None None None Human 7.6 pEC50 = 7.6 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 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 63908 0 None None None Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL13910 63908 0 None None None Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 649 14 3 6 4.4 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1 10.1021/jm025600i
CHEMBL186970 484956 0 None None None Human 6.5 pEC50 = 6.5 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 861 28 10 10 -0.9 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 484981 0 None None None Human 6.5 pEC50 = 6.5 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.2 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 487355 0 None None None Human 5.5 pEC50 = 5.5 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 10 10 -1.2 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 198760 0 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276012 198760 0 None None None Human 5.4 pEC50 = 5.4 Binding
In vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin-3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 546 12 3 6 3.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL365794 487359 0 None None None Human 5.4 pEC50 = 5.4 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 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 487484 0 None None None Human 5.4 pEC50 = 5.4 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 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 333373 0 None None None Human 4.4 pEC50 = 4.4 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 333373 0 None None None Human 4.4 pEC50 = 4.4 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL190080 484964 0 None None None Human 6.3 pEC50 = 6.3 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 932 31 10 10 -0.8 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 484978 0 None None None Human 5.3 pEC50 = 5.3 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 485778 0 None None None Human 5.3 pEC50 = 5.3 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 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 484980 0 None None None Human 6.2 pEC50 = 6.2 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 484963 0 None None None Human 5.2 pEC50 = 5.2 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 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 484969 0 None None None Human 5.2 pEC50 = 5.2 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 8 10 -1.3 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 332923 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 332923 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL365913 487361 0 None None None Human 8.1 pEC50 = 8.1 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 12 10 -1.5 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 40519 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347221 40519 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL124169 40519 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 40519 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322795 473859 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 473859 0 None None None Human 7.2 pEC50 = 7.2 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
11813437 198793 0 None None None Human 5.2 pEC50 = 5.2 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
CHEMBL276301 198793 0 None None None Human 5.2 pEC50 = 5.2 Binding
In vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 3 receptor (MC3R) was determined by a SPA-based cAMP assay in melanoma cells
ChEMBL 530 12 2 5 4.0 CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1 10.1021/jm025600i
44322869 215840 0 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 215840 0 None None None Human 7.1 pEC50 = 7.1 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
46877881 465190 0 None None None Human 6.1 pEC50 = 6.1 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 465190 0 None None None Human 6.1 pEC50 = 6.1 Binding
Inhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsInhibition of human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL190203 484966 0 None None None Human 6.1 pEC50 = 6.1 Binding
Effective concentration against human melanocortin receptor-3 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 484166 0 None None None Human 9.7 pIC50 = 9.7 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
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/jm0202526
44366081 24554 0 None None None Human 9.7 pIC50 = 9.7 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 24554 0 None None None Human 9.7 pIC50 = 9.7 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2096742 484199 0 None None None Human 9.6 pIC50 = 9.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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 488968 0 None None None Human 9.0 pIC50 = 9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1041 16 15 11 -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](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
122194229 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
1324 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
16197727 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
4836 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL3629347 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
CHEMBL441738 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
DB04931 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960840h
122194229 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
1324 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
16197727 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
4836 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL3629347 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
CHEMBL441738 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
DB04931 621 23 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm960845e
127036484 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
1323 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
92432 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL3735690 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
CHEMBL430239 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.5b01285
127036484 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
1323 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
92432 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL3735690 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
CHEMBL430239 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00488
145972289 329453 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 329453 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44418421 327751 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL435923 327751 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 387 5 1 2 4.0 O=C(CCc1c[nH]c2ccccc12)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL393075 487766 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1032 16 14 11 -0.1 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
127036484 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
1323 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
92432 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
CHEMBL3735690 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
CHEMBL430239 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm070461w
127036484 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
1323 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
92432 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
CHEMBL3735690 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
CHEMBL430239 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm801300c
127036484 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
1323 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
92432 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
CHEMBL3735690 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
CHEMBL430239 5482 39 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm0510326
CHEMBL204310 485035 0 None None None Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 908 15 11 9 -0.2 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 241002 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600837 241002 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL413573 488288 0 None None None Human 8.8 pIC50 = 8.8 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 879 13 10 8 1.2 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 488525 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 receptor
ChEMBL 1149 17 13 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](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
127036484 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
1323 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
92432 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL3735690 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
CHEMBL430239 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2006.07.015
133053557 328674 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 328674 0 None None None Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
118735101 237589 0 None None None Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 237589 0 None None None Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL410795 488139 0 None None None Human 6.0 pIC50 = 6 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 237591 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 237591 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44315095 203182 0 None None None Human 5.0 pIC50 = 5 Binding
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL307857 203182 0 None None None Human 5.0 pIC50 = 5 Binding
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 559 13 3 4 4.2 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL410217 488105 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 981 12 13 11 -2.4 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 327664 0 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 327664 0 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
122184635 241007 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600916 241007 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145977650 328799 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 328799 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44445083 310362 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398665 310362 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 953 9 10 9 2.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
101043845 332258 1 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
145948876 332258 1 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299441 332258 1 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL5177536 332258 1 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1220 17 14 11 1.9 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161316 484437 0 None None None Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1048 15 13 10 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](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
44391999 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None None None Human 6.0 pIC50 = 6.0 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
24774602 333565 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL438744 333565 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 766 9 10 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44445085 197396 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL267265 197396 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 879 9 11 9 1.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL425591 488459 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 917 14 11 9 0.5 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 327719 0 None None None Human 6.9 pIC50 = 6.9 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL433764 327719 0 None None None Human 6.9 pIC50 = 6.9 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL382369 487619 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 859 15 11 9 -0.8 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 308745 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 308745 0 None None None Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
176 823 54 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None None None Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL373344 487492 0 None None None Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 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 484959 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.6 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 484966 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 241127 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 241127 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL203760 485032 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 877 12 9 8 1.0 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 241010 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600919 241010 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44348144 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
10188529 6967 6 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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
1337 6967 6 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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 6967 6 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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 6967 6 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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
CHEMBL365401 6967 6 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 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
CHEMBL3350396 486875 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1095 17 14 12 -1.7 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 329293 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212629 329293 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 875 11 12 9 -0.5 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL263822 486104 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 886 16 12 9 -1.6 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 487626 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 909 15 11 9 0.4 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 485793 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 1055 14 10 10 2.3 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]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 241006 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 241006 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44448660 195354 0 None None None Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 195354 0 None None None Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44449216 195644 0 None None None Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL256286 195644 0 None None None Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3600912 487203 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)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 239900 0 None None None Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
CHEMBL358015 239900 0 None None None Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0202526
127053936 298873 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
CHEMBL3968918 298873 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 598 11 2 4 5.7 O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1 nan
2247 1042 63 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL186970 484956 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 861 28 10 10 -0.9 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 329587 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 329587 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44391999 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None None None Human 5.8 pIC50 = 5.8 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
71456245 160468 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 160468 0 None None None Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
171378343 388754 0 None None None Human 6.8 pIC50 = 6.8 Binding
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 388754 0 None None None Human 6.8 pIC50 = 6.8 Binding
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 241129 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601429 241129 0 None None None Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
122184575 241001 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 241001 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
10282847 241526 0 None None None Human 6.8 pIC50 = 6.8 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360819 241526 0 None None None Human 6.8 pIC50 = 6.8 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 5.9 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1 10.1016/j.bmcl.2005.05.012
5624 66319 15 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 66319 15 None None None Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
57854102 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
57854192 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3936968 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
CHEMBL3975851 295005 0 None None None Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 576 11 5 4 4.2 N=C(N)NCCC[C@@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O nan
127053937 295732 0 None None None Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
CHEMBL3942822 295732 0 None None None Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 502 11 2 4 4.3 CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O nan
1800 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10864861 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None None None Rat 5.7 pIC50 = 5.7 Binding
Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL214332 485136 29 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 487199 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 484440 0 None None None Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1096 15 13 10 1.3 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]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
44577514 336975 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577515 336975 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL448081 336975 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508816 336975 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 943 12 11 11 1.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL2112008 485087 0 None None None Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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
CHEMBL6067481 479736 0 None None None Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
1016 8173 46 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None None None Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL365913 487361 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 12 10 -1.5 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 484967 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 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 484968 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 10 10 -1.2 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
127036484 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
1323 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
92432 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
CHEMBL3735690 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
CHEMBL430239 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/ml500436s
127036484 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
1323 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
92432 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL3735690 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
CHEMBL430239 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.ejmech.2018.04.021
127036484 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
1323 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
92432 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
CHEMBL3735690 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
CHEMBL430239 5482 39 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm060768f
CHEMBL503229 489006 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1593 48 23 18 -2.5 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 387810 0 None None None Human 8.7 pIC50 = 8.7 Binding
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 387810 0 None None None Human 8.7 pIC50 = 8.7 Binding
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 488858 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1609 48 21 20 -2.9 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 329191 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4211275 329191 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL502300 488996 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1091 16 15 11 -0.9 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]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL2096742 484199 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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 488985 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1091 16 15 11 -0.9 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]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL3752534 487533 1 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1131 15 12 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL1161320 484439 0 None None None Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1020 15 13 10 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]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
CHEMBL1161323 484441 0 None None None Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1116 15 12 10 2.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
122184637 241009 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 241009 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL204263 485034 0 None None None Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 937 16 12 9 -0.4 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 489128 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 1041 16 15 11 -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](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
122194229 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
1324 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
16197727 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
4836 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL3629347 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
CHEMBL441738 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
DB04931 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm000211e
145975465 328911 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207725 328911 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 825 11 12 9 -1.6 CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
122184910 241128 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601428 241128 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
24774521 310316 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398635 310316 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 861 9 10 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL3600832 487195 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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
44348144 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71449047 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456219 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111807 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112603 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL408336 160025 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44396986 139715 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 139715 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 139715 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 139715 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44408287 157053 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 157053 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
15953838 135872 0 None None None Human 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 135872 0 None None None Human 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-3-receptor (MC3R)
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
168282779 374239 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5188894 374239 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL3600920 487205 0 None None None Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 331848 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 331848 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
127053935 290942 0 None None None Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL3904191 290942 0 None None None Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.
ChEMBL 602 11 2 4 6.2 O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1 nan
CHEMBL217305 484207 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 984 15 11 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](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/s0960-894x(03)00412-8
122184499 240967 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600737 240967 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
24774438 195243 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253789 195243 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 816 9 10 9 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)c2nccnc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
9808801 123573 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 123573 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
44408286 277945 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 277945 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
44391999 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44392015 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44441681 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
6918813 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1187982 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1196338 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL249319 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 27043 2 None None None Human 5.6 pIC50 = 5.6 Binding
Concentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-3 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
ChEMBL 557 7 3 5 2.9 CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
168273822 373658 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 373658 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
122184578 241004 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600839 241004 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL217584 485224 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1095 17 14 12 -1.7 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 1895 54 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None None None Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
168285801 374542 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5193501 374542 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
44347840 317432 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
91932630 317432 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL415333 317432 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0202526
CHEMBL2096759 485069 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 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 485126 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1095 17 14 12 -1.7 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 487587 0 None None None Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 843 15 10 8 0.6 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 328925 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 328925 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3600834 487197 0 None None None Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1088 17 13 11 0.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)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 485796 0 None None None Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 1015 12 8 9 2.8 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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL203602 485031 0 None None None Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 858 15 11 9 -1.4 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 487607 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 827 12 9 8 -0.1 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 486807 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 213911 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
CHEMBL309807 213911 0 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 3 receptor (hMC3R) using [125I]NDP-alpha-MSH as radioligand
ChEMBL 601 14 5 4 3.7 CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1 10.1016/s0960-894x(03)00412-8
44431512 292638 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 292638 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL2372588 485878 0 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1082 15 12 10 1.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
90643832 221245 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/acs.jmedchem.4c00110
CHEMBL3287339 221245 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 784 15 8 7 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/acs.jmedchem.4c00110
44348144 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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
71449047 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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
71456219 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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
CHEMBL408336 160025 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1533 33 16 22 -1.3 CC(=O)[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
44349173 235857 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
44383343 235857 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
CHEMBL338768 235857 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
CHEMBL353007 235857 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/j.bmcl.2003.10.056
44448631 195446 0 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 195446 0 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44448590 195963 0 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 195963 0 None None None Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL2371712 485760 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1588 44 18 19 -0.8 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 196977 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL263585 196977 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1561 33 16 22 -0.6 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3600835 487198 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 484199 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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
122194229 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
1324 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
16197727 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
4836 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL3629347 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
CHEMBL441738 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
DB04931 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm049579s
122194229 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
1324 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
16197727 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
4836 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL3629347 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL441738 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
DB04931 621 23 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm030111j
CHEMBL266417 484238 0 None None None Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human Melanocortin 3 receptorInhibitory activity against human Melanocortin 3 receptor
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)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 484279 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=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
122194229 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
1324 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
16197727 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
4836 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
CHEMBL3629347 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
CHEMBL441738 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
DB04931 621 23 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against Melanocortin 3 receptorInhibitory activity against Melanocortin 3 receptor
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm00018a005
145964017 328999 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 328999 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL214332 485136 29 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 485136 29 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 488020 0 None None None Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1627 47 20 19 -0.7 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 375345 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 375345 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
44348183 197480 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL268094 197480 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1493 31 14 21 -0.8 CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44408173 157068 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL203975 157068 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 640 8 2 5 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL188738 484961 0 None None None Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 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 241525 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL360818 241525 0 None None None Human 7.5 pIC50 = 7.5 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.7 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1 10.1016/j.bmcl.2005.05.012
163196518 375167 5 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5203580 375167 5 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
24774519 195242 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL253788 195242 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 911 9 10 8 2.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL2310901 485337 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1523 44 18 17 -1.2 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 123582 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762009 123582 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 587 6 3 4 4.7 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3601426 487208 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 39502 6 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 39502 6 None None None Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL3349030 486807 0 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 164667 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218748 164667 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
10077258 38929 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 38929 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
3198 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None None None Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL3600842 487201 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 311234 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402769 311234 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.2 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2008.04.049
24858629 390311 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL552520 390311 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 853 10 9 10 1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44408155 277834 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL381125 277834 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 656 10 2 5 4.9 CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.11.095
44445082 310359 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL398664 310359 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 799 9 10 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
54586246 123581 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1762008 123581 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 599 8 3 4 5.0 CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL2371967 485797 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 1077 12 8 9 3.8 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]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0614275
CHEMBL190732 484969 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 8 10 -1.3 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 485781 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 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 487359 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 9 10 -1.3 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 329656 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4217528 329656 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 929 11 12 9 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44577510 371922 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44577523 371922 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 371922 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL508068 371922 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL437050 484343 3 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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
CHEMBL1775066 484791 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 992 15 15 10 -1.6 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 277611 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 277611 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44277696 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44372933 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
70695694 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL2111251 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL349298 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 3 receptor using radiolabeled NDP-MSH displacement
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
44277696 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
44372933 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
70695694 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL2111251 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL349298 159974 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC3R by using radioligand NDP-MSH
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL1161318 484438 0 None None None Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1062 15 13 10 1.5 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](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
44397220 327654 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 327654 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL3600841 487200 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 160466 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 160466 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
16725559 195368 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254757 195368 0 None None None Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
44431513 292523 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391704 292523 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1054 14 12 10 1.4 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
44348200 315941 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL410949 315941 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1511 33 16 22 -1.7 CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C 10.1021/jm030111j
CHEMBL3348530 486805 0 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human melanocortin 3 receptorInhibitory activity against human melanocortin 3 receptor
ChEMBL 983 16 13 11 -0.8 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 477720 0 None None None Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 1055 12 8 9 3.6 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]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O 10.1021/jm0614275
CHEMBL439691 488789 0 None None None Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1567 47 21 20 -3.1 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 375378 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5206941 375378 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2cccc(c2)CSC1(C)C 10.1021/acs.jmedchem.1c01848
168273291 373619 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
CHEMBL5179637 373619 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1163 17 13 12 3.0 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)C(C)(C)SCc2ccccc2CSC1(C)C 10.1021/acs.jmedchem.1c01848
145987870 332026 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4292317 332026 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 620 14 5 5 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44408190 197247 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL265985 197247 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 606 8 2 5 4.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL3600833 487196 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 486807 0 None None None Human 6.3 pIC50 = 6.3 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 38940 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 38940 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
71459938 160473 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 160473 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44397455 251902 0 None None None Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL362523 251902 0 None None None Human 7.3 pIC50 = 7.3 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 620 7 3 4 5.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL417853 488420 0 None None None Human 4.3 pIC50 = 4.3 Binding
Inhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligandInhibitory activity against hMC3R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligand
ChEMBL 557 15 4 5 1.9 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 39036 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 39036 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of human melanocortin 3 receptorInhibition of human melanocortin 3 receptor
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44408276 157173 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL204308 157173 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 632 8 2 5 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862425 38958 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 38958 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
44418431 270465 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL373821 270465 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL413439 488283 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1602 47 21 18 -1.3 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 329252 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 329252 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44431511 178928 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL234629 178928 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC3R expressed in HEK293 cells
ChEMBL 1004 14 12 10 0.3 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
178316117 466515 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 806 25 9 7 3.2 CCCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.4c00110
CHEMBL6147624 466515 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 806 25 9 7 3.2 CCCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O 10.1021/acs.jmedchem.4c00110
CHEMBL263948 486113 2 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM
ChEMBL 1664 50 22 22 -4.7 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](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
CHEMBL214332 485136 29 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=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 484790 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 992 15 15 10 -1.6 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 237588 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 237588 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL191120 484981 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.2 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 484980 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 487484 0 None None None Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 11 10 -1.6 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 487206 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 277946 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 277946 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL3600913 487204 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 329563 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 329563 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL264190 484234 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 685 18 10 7 -0.4 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.4c00110
CHEMBL446185 488874 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 867 14 11 9 -0.6 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 160026 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456220 160026 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 160026 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 160026 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
145966490 329307 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212762 329307 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 839 11 12 9 -1.2 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
145948912 332260 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 332260 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
122184914 241132 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 241132 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
145966364 329073 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 329073 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL3754655 487540 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
ChEMBL 1081 15 12 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.5b01285
CHEMBL414778 488367 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1578 47 20 20 -2.5 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 488753 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1578 47 20 20 -2.5 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 485037 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 893 15 10 8 1.7 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
CHEMBL405282 487855 22 None None None Human 8.2 pIC50 = 8.2 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 484227 0 None None None Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human Melanocortin-3 receptorBinding affinity for human Melanocortin-3 receptor
ChEMBL 1096 15 12 10 1.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL405282 487855 22 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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 488473 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 829 13 10 8 0.0 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 241131 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 241131 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3349030 486807 0 None None None Human 6.2 pIC50 = 6.2 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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
44577519 371951 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
44577520 371951 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL505536 371951 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL506274 371951 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells
ChEMBL 904 12 10 11 1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm701181n
CHEMBL411359 488169 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1552 47 21 18 -2.5 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 139478 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL187774 139478 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44396986 139715 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71452720 139715 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 139715 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 139715 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
71449048 160026 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
71456220 160026 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2111808 160026 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL2112604 160026 0 None None None Human 6.2 pIC50 = 6.2 Binding
Inhibition of human Melanocortin 3 receptorInhibition of human Melanocortin 3 receptor
ChEMBL 1483 33 16 22 -2.5 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL264190 484234 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 685 18 10 7 -0.4 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 484234 0 None None None Human 7.2 pIC50 = 7.2 Binding
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 685 18 10 7 -0.4 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 277631 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 277631 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL2371963 485794 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 1001 12 8 9 2.4 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]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm0614275
CHEMBL190080 484964 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 932 31 10 10 -0.8 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 375277 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 375277 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL3600843 487202 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 123572 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 123572 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
10257242 38928 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 38928 0 None None None Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL3601431 487209 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 333518 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 333518 0 None None None Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
178295274 466882 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.4c00110
CHEMBL6163235 466882 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of MC3R (unknown origin)Inhibition of MC3R (unknown origin)
ChEMBL 822 18 9 7 0.9 CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.4c00110
168278924 374139 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5187368 374139 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL437050 484343 3 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
ChEMBL 1570 47 21 19 -2.9 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
CHEMBL437050 484343 3 None None None Human 7.1 pIC50 = 7.1 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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
CHEMBL3349030 486807 0 None None None Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 328725 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 328725 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
168274393 373202 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5172938 373202 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
54584302 123576 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761874 123576 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1 10.1016/j.bmcl.2011.02.090
54584301 123574 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
CHEMBL1761872 123574 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 585 6 2 4 4.6 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C 10.1016/j.bmcl.2011.02.090
44408154 278594 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
CHEMBL383719 278594 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 668 8 2 5 5.1 CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O 10.1016/j.bmcl.2005.11.095
10864861 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10886436 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10952071 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
1338 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
9938402 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL140108 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL334457 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL339053 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
CHEMBL342954 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.05.012
10864861 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10886436 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10952071 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL140108 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL334457 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL342954 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
10864861 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10886436 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
10952071 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL140108 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL334457 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL342954 8293 40 None None None Human 6.1 pIC50 = 6.1 Binding
Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
49862375 38937 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209318 38937 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1 10.1016/j.bmcl.2010.06.038
CHEMBL190953 484978 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 10 10 -1.3 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 486330 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 904 29 9 10 -1.3 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 487489 0 None None None Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-3 expressed in 293 HEK cells
ChEMBL 918 30 11 10 -1.2 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 241003 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 241003 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1016/j.bmcl.2011.03.019
122184636 241008 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 241008 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
127036484 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
1323 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
92432 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
CHEMBL3735690 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
CHEMBL430239 5482 39 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/jm960845e
CHEMBL3349030 486807 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity for Human Melanocortin 3 receptor expressed in L-cellsBinding affinity for Human Melanocortin 3 receptor expressed in L-cells
ChEMBL 1570 47 21 19 -2.9 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 488047 0 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against hMC3R transfected in HEK293 cellsInhibitory activity against hMC3R transfected in HEK293 cells
ChEMBL 895 14 11 9 0.0 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 139528 0 None None None Human 7.1 pIC50 = 7.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL187990 139528 0 None None None Human 7.1 pIC50 = 7.1 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 606 7 3 4 5.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
44445084 316349 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
CHEMBL411391 316349 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 829 9 11 9 0.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44408275 157086 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL204078 157086 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 620 8 2 5 5.1 C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL375947 487549 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 964 13 10 10 0.2 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 38939 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 38939 0 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
11753695 22707 5 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 22707 5 None None None Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
122184633 241005 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600914 241005 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
127036484 5482 39 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
1323 5482 39 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
92432 5482 39 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL3735690 5482 39 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
CHEMBL430239 5482 39 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c01848
145990599 331665 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4285535 331665 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis
ChEMBL 710 17 7 6 2.6 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44397410 252385 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363740 252385 0 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 3 receptor expressed in CHO cells
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
10188529 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL365401 6967 6 None None None Human 6.0 pIC50 = 6.0 Binding
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
10304776 160471 0 None None None Human 7.0 pIC50 = 7.0 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
CHEMBL2113041 160471 0 None None None Human 7.0 pIC50 = 7.0 Binding
Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells
ChEMBL 634 7 3 4 6.1 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1 10.1016/j.bmcl.2005.05.012
10483153 123575 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 123575 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in CHO cells
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL3600922 487207 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC3 receptor expressed in HEK293 cells after 40 mins by luminescence counting
ChEMBL 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)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 487742 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC3R expressed in CHO cells
ChEMBL 964 13 10 10 0.2 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 24554 0 None -2 2 Human 9.4 pKd = 9.4 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL1161313 24554 0 None -2 2 Human 9.4 pKd = 9.4 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1036 15 13 11 0.4 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O 10.1021/jm0202526
CHEMBL2372589 484227 0 None 15 2 Human 9.2 pKd = 9.2 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1096 15 12 10 1.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1021/jm0202526
CHEMBL1161322 484166 0 None -1 2 Human 9.0 pKd = 9 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
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/jm0202526
CHEMBL2096742 484199 0 None -5 2 Human 8.7 pKd = 8.7 Binding
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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 484439 0 None 12 2 Human 7.6 pKd = 7.6 Binding
pA2 value for human melanocortin receptor Melanocortin-3 receptorpA2 value for human melanocortin receptor Melanocortin-3 receptor
ChEMBL 1020 15 13 10 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]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O 10.1021/jm0202526
CHEMBL1161318 484438 0 None -79 2 Human 6.5 pKd = 6.5 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1062 15 13 10 1.5 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](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O 10.1021/jm0202526
CHEMBL1161321 484440 0 None -19 2 Human 6.4 pKd = 6.4 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1096 15 13 10 1.3 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]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O 10.1021/jm0202526
CHEMBL440801 488809 0 None -25 2 Human 8.3 pKd = 8.3 Binding
pA2 against human melanocortin receptor, hMC3RpA2 against human melanocortin receptor, hMC3R
ChEMBL 1149 17 13 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](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303103
CHEMBL2096742 484199 0 None -5 2 Human 8.3 pKd = 8.3 Binding
pA2 value for the compound against human Melanocortin 3 receptorpA2 value for the compound against human Melanocortin 3 receptor
ChEMBL 1074 17 14 11 0.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=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 484441 0 None -5 2 Human 8.2 pKd = 8.2 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1116 15 12 10 2.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O 10.1021/jm0202526
CHEMBL1161316 484437 0 None -63 2 Human 6.2 pKd = 6.2 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1048 15 13 10 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](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 485878 0 None -316 2 Human 6.1 pKd = 6.1 Binding
pA2 value for human Melanocortin-3 receptorpA2 value for human Melanocortin-3 receptor
ChEMBL 1082 15 12 10 1.6 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O 10.1021/jm0202526
162643092 355566 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 355566 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643092 355566 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4777048 355566 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 366417 0 None -1 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 366417 0 None -1 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673650 366417 0 None -1 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794121 366417 0 None -1 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 366791 0 None -2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 366791 0 None -2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162676295 366791 0 None -2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4798971 366791 0 None -2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL414718 488362 0 None -1 4 Human 10.0 pKi = 10.0 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1846 55 24 24 -5.9 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
127035019 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
1325 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
9898183 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3735607 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
127035019 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
1325 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
9898183 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3422426 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
CHEMBL3735607 7320 11 None -5 4 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10.1021/acs.jmedchem.0c01620
162673931 366422 0 None -8 2 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 366422 0 None -8 2 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673931 366422 0 None -8 2 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794168 366422 0 None -8 2 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL2370968 485651 0 None 1 3 Human 9.7 pKi = 9.7 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1561 44 19 17 -1.4 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 484358 0 None -3 3 Human 9.6 pKi = 9.6 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)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 488387 0 None -2 5 Human 9.6 pKi = 9.6 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 2006 60 27 28 -7.9 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)CC(N)=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(=O)NCC(=O)O)C(C)C 10.1021/jm0501432
162668987 356405 0 None -15 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 356405 0 None -15 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162668987 356405 0 None -15 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4788071 356405 0 None -15 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 366485 0 None -13 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 366485 0 None -13 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672763 366485 0 None -13 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4794990 366485 0 None -13 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1092 17 14 11 0.3 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 366249 0 None -13 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 366249 0 None -13 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672255 366249 0 None -13 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 366249 0 None -13 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 366387 0 None -18 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 366387 0 None -18 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672837 366387 0 None -18 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793821 366387 0 None -18 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1098 17 13 13 0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168277761 373394 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175981 373394 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2342 37 34 29 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
122194229 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
1324 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
16197727 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
4836 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
CHEMBL3629347 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
CHEMBL441738 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
DB04931 621 23 None -4 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1016/s0960-894x(03)00552-3
162677133 366892 0 None -19 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 366892 0 None -19 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162677133 366892 0 None -19 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4800268 366892 0 None -19 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1108 17 14 11 0.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
122194229 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
1324 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
16197727 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
4836 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL3629347 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL441738 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
DB04931 621 23 None -4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10.1021/jm201489a
CHEMBL2370964 485647 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1601 47 21 18 -1.9 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
127036484 5482 39 None -48 4 Human 9.0 pKi = 9.0 Binding
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
1323 5482 39 None -48 4 Human 9.0 pKi = 9.0 Binding
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
92432 5482 39 None -48 4 Human 9.0 pKi = 9.0 Binding
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL3735690 5482 39 None -48 4 Human 9.0 pKi = 9.0 Binding
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL430239 5482 39 None -48 4 Human 9.0 pKi = 9.0 Binding
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 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c01587
CHEMBL385465 487662 0 None -10 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 960 12 12 10 -0.8 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 161412 0 None -2 3 Human 9.0 pKi = 9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 161412 0 None -2 3 Human 9.0 pKi = 9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415914 276593 0 None -1 3 Human 9.0 pKi = 9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 276593 0 None -1 3 Human 9.0 pKi = 9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415919 278801 0 None -2 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385000 278801 0 None -2 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 780 16 6 7 1.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL2370154 477645 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 1038 17 14 11 -0.6 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 486215 0 None -6 4 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1322 40 18 16 -2.9 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
11993702 484262 27 None -3 3 Human 8.0 pKi = 8 Binding
Agonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysisAgonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
CHEMBL3301624 484262 27 None -3 3 Human 8.0 pKi = 8 Binding
Agonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysisAgonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
DB11700 484262 27 None -3 3 Human 8.0 pKi = 8 Binding
Agonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysisAgonist activity at human MC3R expressed in CHO-K1 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.4c01556
162665450 356123 0 None -10 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 356123 0 None -10 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162665450 356123 0 None -10 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4784053 356123 0 None -10 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
168273645 373418 0 None -24 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5176443 373418 0 None -24 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 5162 106 68 67 -6.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL412536 488230 18 None -12 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 2659 85 36 37 -10.0 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)N)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(=O)O 10.1021/jm0501432
168289404 374377 0 None -15 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 374377 0 None -15 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5087814 479290 0 None -26 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1859 20 19 19 1.7 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 140911 0 None -416 2 Human 6.0 pKi = 6 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL191857 140911 0 None -416 2 Human 6.0 pKi = 6 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 615 10 3 5 5.7 CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
9915636 139111 0 None -58 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186083 139111 0 None -58 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44434860 180870 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238159 180870 0 None -3 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL5094168 479635 0 None -707 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1994 29 24 22 -0.7 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 479450 0 None -75 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1827 23 24 21 -1.6 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 273113 0 None -3 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL372965 273113 0 None -3 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 630 13 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
176 823 54 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 823 54 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 823 54 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 823 54 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 823 54 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
59149264 158448 0 None -85 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 158448 0 None -85 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 158448 0 None -85 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 158448 0 None -85 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168277916 373761 0 None -17 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5181812 373761 0 None -17 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4986 94 68 63 -6.6 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168272660 373521 0 None -14 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 373521 0 None -14 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322869 215840 0 None 6 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313690 215840 0 None 6 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 867 11 12 9 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322895 328350 0 None -18 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 328350 0 None -18 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168285313 374465 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 374465 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44433294 309191 0 None -575 3 Human 6.0 pKi = 6.0 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL397580 309191 0 None -575 3 Human 6.0 pKi = 6.0 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 619 11 2 5 4.6 CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL2070254 477530 0 None -31 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2023 62 26 26 -1.9 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 139652 0 None -131 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL188651 139652 0 None -131 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 607 11 3 6 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
6918850 253432 0 None -316 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
CHEMBL364560 253432 0 None -316 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1 10.1016/j.bmcl.2005.05.017
10270570 179891 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236450 179891 0 None -2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 6 2 2 4.4 CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44401592 253205 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL364519 253205 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 607 13 6 4 3.2 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
46905545 24591 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161792 24591 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 631 14 7 6 1.4 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44415972 161345 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 161345 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL5078687 478768 0 None -75 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1853 23 23 21 -1.1 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 270514 0 None -91 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 270514 0 None -91 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
51346770 121017 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
CHEMBL1682209 121017 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 643 11 2 8 3.5 COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O 10.1016/j.bmcl.2011.01.011
44413876 161208 0 None -93 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL211699 161208 0 None -93 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44413876 161208 0 None -93 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL211699 161208 0 None -93 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 710 18 8 7 0.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O 10.1021/jm060384p
CHEMBL2370967 485650 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1612 47 20 18 -1.2 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 40519 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347221 40519 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL124169 40519 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL432377 40519 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44347331 40216 0 None -181 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None -181 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
16007264 161185 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL211564 161185 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
16007264 161185 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
CHEMBL211564 161185 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 572 9 2 4 5.5 CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1021/jm701137s
71452732 160524 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113139 160524 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 697 8 2 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
71461657 160529 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
CHEMBL2113144 160529 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 556 6 2 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.07.035
44435220 180103 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236803 180103 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 10 2 3 8.9 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1 10.1016/j.bmc.2007.06.003
10293285 180441 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL237528 180441 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 382 7 1 2 4.9 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
10137615 180565 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237692 180565 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 9 2 2 5.4 CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 180858 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434766 310744 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 310744 0 None -10 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
59149266 158570 0 None -707 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693081 158570 0 None -707 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929807 158570 0 None -707 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070250 158570 0 None -707 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
168296647 375502 0 None -190 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 375502 0 None -190 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
11845813 277109 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 277109 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
10864861 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
10886436 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
10952071 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
1338 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL140108 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL334457 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL342954 8293 40 None -75 4 Human 6.9 pKi = 6.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
44413829 159644 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210011 159644 0 None -10 3 Human 5.9 pKi = 5.9 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
25133556 372025 0 None -23 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 372025 0 None -23 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
44569175 372002 0 None -32 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 372002 0 None -32 3 Human 6.9 pKi = 6.9 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
168277543 373759 0 None -128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5181752 373759 0 None -128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
59149255 158572 0 None -50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 158572 0 None -50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 158572 0 None -50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 158572 0 None -50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11993702 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
DB11700 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.2c00793
11993702 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 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 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 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 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
DB11700 484262 27 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 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 1116 18 17 14 -2.8 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](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.1c00095
168276507 373359 0 None -33 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 373359 0 None -33 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
10033237 141334 0 None -79 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44322896 141334 0 None -79 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL1923662 141334 0 None -79 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 141334 0 None -79 4 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168293710 375204 0 None -56 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 375204 0 None -56 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322958 216665 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 216665 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44432932 178618 0 None -38 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233758 178618 0 None -38 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 574 14 2 6 6.6 CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44400863 141426 0 None -288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192464 141426 0 None -288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 602 11 2 6 5.8 CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44456219 308755 0 None -275 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL403806 308755 0 None -275 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
16046215 161548 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
CHEMBL213122 161548 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1016/j.bmcl.2006.06.075
16046215 161548 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
CHEMBL213122 161548 0 None -51 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 441 7 1 3 5.2 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1 10.1021/jm701137s
44434843 179559 0 None -3 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 179559 0 None -3 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434854 180857 0 None -8 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 180857 0 None -8 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434648 294846 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393558 294846 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.1 NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
172441600 387613 0 None -288 3 Human 6.9 pKi = 6.9 Binding
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 387613 0 None -288 3 Human 6.9 pKi = 6.9 Binding
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 374705 0 None -190 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 374705 0 None -190 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5080489 478873 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1811 21 23 21 -2.2 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 1042 63 None -109 37 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 1042 63 None -109 37 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 1042 63 None -109 37 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 1042 63 None -109 37 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 1042 63 None -109 37 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44401573 143428 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL195638 143428 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 568 13 5 4 2.8 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL420167 488424 0 None -8 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 918 11 12 10 -0.9 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 484238 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)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 332923 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
CHEMBL433413 332923 0 None 4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 871 27 12 10 -1.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm020021z
44322787 215649 0 None -12 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL312998 215649 0 None -12 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 791 21 11 8 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370965 485648 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1586 47 19 17 -0.7 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 180752 0 None -165 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL237976 180752 0 None -165 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44323212 333373 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
CHEMBL436903 333373 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 787 9 10 8 -1.0 C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm020021z
11180881 139108 1 None -93 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
CHEMBL186074 139108 1 None -93 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 593 11 3 6 4.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1 10.1016/j.bmcl.2004.08.055
44395681 139157 0 None -100 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL186289 139157 0 None -100 4 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 567 13 3 6 3.8 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
44415417 161605 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL213380 161605 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 465 7 1 3 5.5 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
10304463 158422 0 None -14 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL206840 158422 0 None -14 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 615 11 1 5 5.6 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.10.103
9915636 139111 0 None -58 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL186083 139111 0 None -58 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 553 12 3 6 3.5 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44265715 24484 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159702 24484 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
10108894 180566 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
CHEMBL237693 180566 0 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 355 8 2 2 4.4 NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1 10.1016/j.bmc.2007.06.003
44434697 295373 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL393994 295373 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 543 10 2 4 6.8 COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434757 299364 0 None -7 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397324 299364 0 None -7 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 2 4 8.3 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
126736894 366943 28 None -616 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3R assessed as inhibition constantBinding affinity to human MC3R assessed as inhibition constant
ChEMBL 675 9 1 6 6.0 COC[C@H]1CN(C(=O)[C@]2(F)CN(C3CCCC3)C[C@H]2c2ccc(OC)cc2)C[C@@H]1c1ccc(C(F)(F)F)cc1N1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.4c02358
CHEMBL4802160 366943 28 None -616 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to human MC3R assessed as inhibition constantBinding affinity to human MC3R assessed as inhibition constant
ChEMBL 675 9 1 6 6.0 COC[C@H]1CN(C(=O)[C@]2(F)CN(C3CCCC3)C[C@H]2c2ccc(OC)cc2)C[C@@H]1c1ccc(C(F)(F)F)cc1N1CCC(C(=O)O)CC1 10.1021/acs.jmedchem.4c02358
25129105 350974 0 None -23 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 350974 0 None -23 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL5081077 478899 0 None -30 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1983 30 28 23 -3.8 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 389138 0 None -912 3 Human 6.8 pKi = 6.8 Binding
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 389138 0 None -912 3 Human 6.8 pKi = 6.8 Binding
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 252065 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL362964 252065 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 621 14 6 4 3.3 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413913 276031 0 None -2 3 Human 5.8 pKi = 5.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 276031 0 None -2 3 Human 5.8 pKi = 5.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL2370963 485646 0 None -10 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1562 47 20 18 -2.4 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 366217 0 None -33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 366217 0 None -33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162670951 366217 0 None -33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 366217 0 None -33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
42630327 311799 1 None -5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 311799 1 None -5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL407809 487986 0 None -56 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1356 25 18 17 -2.8 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 488045 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1555 30 20 19 -2.5 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 488705 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1668 35 21 20 -1.9 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 40465 0 None -301 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
CHEMBL123938 40465 0 None -301 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 0.2 NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
44347105 232395 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL331728 232395 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 724 9 10 7 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
11375529 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44393441 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL185195 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL351400 138721 0 None -1 4 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434662 179372 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235137 179372 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.6 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434781 180732 0 None -15 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 180732 0 None -15 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
5624 66319 15 None -45 10 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 66319 15 None -45 10 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
44413970 270536 0 None -34 3 Human 4.8 pKi = 4.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 270536 0 None -34 3 Human 4.8 pKi = 4.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413938 276278 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 276278 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44569176 337063 0 None -30 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 337063 0 None -30 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
11846669 161733 0 None -5 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 161733 0 None -5 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
168271934 373182 0 None -9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 373182 0 None -9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
127036484 5482 39 None -48 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
1323 5482 39 None -48 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
92432 5482 39 None -48 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL3735690 5482 39 None -48 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL430239 5482 39 None -48 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.8b00170
44322977 221066 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 221066 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44577092 352556 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467586 352556 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 10 2 5 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL427629 488478 0 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 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 289751 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 289751 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human MC3 receptorBinding affinity at human MC3 receptor
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44400661 252365 0 None -512 2 Human 5.8 pKi = 5.8 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
CHEMBL363641 252365 0 None -512 2 Human 5.8 pKi = 5.8 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 620 11 2 5 6.1 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1 10.1016/j.bmcl.2005.03.053
70693083 158573 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929813 158573 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070253 158573 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1996 61 24 26 -1.3 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44434636 180144 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236841 180144 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 469 12 3 3 5.6 NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
9946241 180272 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237079 180272 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 5 2 2 3.1 NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434782 180855 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238144 180855 0 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 511 10 2 2 7.5 NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434693 332134 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL429451 332134 0 None -7 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 559 12 2 4 7.4 CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
10211466 333537 0 None -213 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL438432 333537 0 None -213 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.1 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
1800 473856 65 None -54 34 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
4189 473856 65 None -54 34 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 473856 65 None -54 34 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
DB01110 473856 65 None -54 34 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44409257 277864 0 None -67 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL381357 277864 0 None -67 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
25133210 334033 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 334033 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL427666 488485 0 None -60 4 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1368 41 18 17 -2.6 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
CHEMBL6067481 479736 0 None 1 3 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL None None None None nan
168273045 373348 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5175392 373348 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2905 62 33 37 -5.8 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415920 161825 0 None -13 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 161825 0 None -13 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44322959 312000 0 None -8 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 312000 0 None -8 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
25132864 337116 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
CHEMBL449050 337116 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 590 12 2 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC 10.1021/jm800525p
25058412 372568 0 None -208 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL513404 372568 0 None -208 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.8 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434587 180277 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237094 180277 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 6 2 3 3.9 NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434848 179826 0 None -11 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL236443 179826 0 None -11 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44434690 180150 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -19 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434713 180425 0 None -14 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 180425 0 None -14 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
10109225 310705 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL399624 310705 0 None -10 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 3 3.2 NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44409240 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
CHEMBL202699 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2005.12.005
44409240 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
CHEMBL202699 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1016/j.bmcl.2006.05.087
44409240 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
CHEMBL202699 156110 0 None -16 3 Human 5.8 pKi = 5.8 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 736 18 8 7 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O 10.1021/jm060384p
172449425 388312 0 None -2818 3 Human 6.8 pKi = 6.8 Binding
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 388312 0 None -2818 3 Human 6.8 pKi = 6.8 Binding
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 8173 46 None -56 35 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 8173 46 None -56 35 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 8173 46 None -56 35 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 8173 46 None -56 35 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 8173 46 None -56 35 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL5075506 478577 0 None -1348 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1925 26 23 22 -0.9 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 315551 0 None -63 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 315551 0 None -63 3 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
127036484 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
1323 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
92432 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL3735690 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL430239 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.2c00793
127036484 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
1323 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
92432 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL3735690 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL430239 5482 39 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.1c00095
44396002 252795 0 None -43 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
CHEMBL364215 252795 0 None -43 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 587 11 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1 10.1016/j.bmcl.2004.08.055
11181804 256447 0 None -158 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 256447 0 None -158 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
23661656 180153 0 None -323 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434575 180153 0 None -323 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236872 180153 0 None -323 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 180153 0 None -323 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434661 179371 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL235136 179371 0 None -4 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 11 2 3 4.4 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.06.003
44434603 180741 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237935 180741 0 None -2 4 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 409 10 2 2 4.9 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265496 197371 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 197371 0 None -13 4 Human 4.8 pKi = 4.8 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
44409379 158176 0 None -85 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL206018 158176 0 None -85 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
25132525 350685 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
CHEMBL460142 350685 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 8 2 4 2.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O 10.1021/jm800525p
168270124 373056 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 373056 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL407213 487949 0 None -44 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 823 10 10 8 -0.2 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 352578 0 None -56 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467772 352578 0 None -56 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 532 10 2 5 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C 10.1016/j.bmc.2008.03.072
10408 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 137257 0 None -301 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL182277 137257 0 None -301 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 642 10 4 6 4.4 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL88185 489400 0 None -11 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 721 19 9 8 -1.2 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 290574 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
CHEMBL390130 290574 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 3 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2004.08.055
10283036 277531 0 None -331 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380540 277531 0 None -331 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 647 11 2 5 5.2 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1 10.1016/j.bmcl.2005.10.103
11296732 290574 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL390130 290574 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 539 11 3 6 3.1 NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44434772 179456 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434621 293015 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL392094 293015 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 561 9 1 5 6.4 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
9969456 294313 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393125 294313 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.7 NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434845 294595 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393350 294595 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 527 10 4 2 6.5 N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
71454518 160640 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL2113315 160640 0 None -12 4 Human 4.7 pKi = 4.7 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 456 10 4 3 3.3 NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
11845444 161527 0 None -11 3 Human 4.7 pKi = 4.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 161527 0 None -11 3 Human 4.7 pKi = 4.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
137631599 312447 0 None -288 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 312447 0 None -288 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11847001 161685 0 None -138 3 Human 5.7 pKi = 5.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213747 161685 0 None -138 3 Human 5.7 pKi = 5.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
156010247 351026 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
CHEMBL4633001 351026 0 None -11 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 2913 40 44 46 -16.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.0c00485
10408 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 1486 31 None -26 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1025 17 13 11 -0.6 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 158565 0 None -5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 158565 0 None -5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57646441 158564 0 None -20 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 158564 0 None -20 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL408843 488035 0 None -6 3 Human 8.6 pKi = 8.6 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1125 15 14 14 -1.6 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 477660 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1538 26 17 20 -2.0 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 486767 0 None -70 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 936 15 11 9 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](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm010165y
44323029 474096 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL92481 474096 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 795 20 10 7 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168284733 374685 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5195641 374685 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2054 33 32 24 -4.1 CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44577062 385891 0 None -48 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL525177 385891 0 None -48 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 4.6 CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11296600 241507 0 None -309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 241507 0 None -309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
10180932 180247 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237051 180247 0 None -3 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 11 2 2 5.8 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434695 180266 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237070 180266 0 None -8 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 503 9 2 2 7.1 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434766 310744 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL399810 310744 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 510 9 2 3 6.9 N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
25128749 352383 0 None -25 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 352383 0 None -25 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
44416152 162543 0 None -38 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215576 162543 0 None -38 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 560 11 3 4 2.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
25129109 371891 0 None -34 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 371891 0 None -34 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
44322812 221867 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 221867 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434584 298579 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL396638 298579 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 3 4.9 NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 179456 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -21 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434690 180150 0 None -19 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -19 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
10291369 333557 0 None -3 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438672 333557 0 None -3 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
2726 1895 54 None -158 48 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 1895 54 None -158 48 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 1895 54 None -158 48 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 1895 54 None -158 48 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 1895 54 None -158 48 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
25132867 337017 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 337017 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
44413932 274948 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 274948 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL2070244 485054 0 None -21 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1543 35 24 20 -7.2 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 352557 0 None -275 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467587 352557 0 None -275 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 548 9 2 5 4.7 COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1 10.1016/j.bmc.2008.03.072
11341045 138459 0 None -123 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 138459 0 None -123 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
44434760 179375 0 None -7 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235140 179375 0 None -7 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 519 9 2 2 7.6 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434691 180265 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL237069 180265 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 11 2 4 7.0 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434701 180332 0 None -16 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL237291 180332 0 None -16 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 499 9 2 2 7.3 Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
44434778 180572 0 None -27 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -27 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434655 180850 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238135 180850 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 12 2 2 5.6 C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434855 180858 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -10 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
168283984 374312 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190172 374312 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2937 64 35 39 -7.9 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44415956 279139 0 None -17 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
CHEMBL387246 279139 0 None -17 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1016/j.bmcl.2006.05.087
44415956 279139 0 None -17 3 Human 4.7 pKi = 4.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL387246 279139 0 None -17 3 Human 4.7 pKi = 4.7 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 531 13 6 5 0.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
44409103 277414 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
CHEMBL380120 277414 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 628 15 5 6 2.4 CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N 10.1016/j.bmcl.2005.12.005
168283616 374306 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5190042 374306 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2110 33 32 25 -4.5 CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44323015 220935 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL327450 220935 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 731 20 9 8 -0.2 CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
23635107 182366 0 None -81 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
CHEMBL240571 182366 0 None -81 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1021/jm070806a
23635107 182366 0 None -81 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240571 182366 0 None -81 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 516 9 2 4 4.3 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C 10.1016/j.bmc.2008.03.072
11477853 139182 0 None -63 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
CHEMBL186439 139182 0 None -63 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 7 3 3 5.2 CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1 10.1021/jm0400496
44562414 350776 0 None -95 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL460942 350776 0 None -95 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 532 10 2 5 3.9 CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
10864861 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
10886436 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
10952071 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
1338 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
9938402 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL140108 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL334457 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL339053 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
CHEMBL342954 8293 40 None -75 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2004.06.059
44394079 254735 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL365278 254735 0 None -85 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 653 11 3 5 4.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
9867330 198143 0 None -100 2 Human 5.6 pKi = 5.6 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 198143 0 None -100 2 Human 5.6 pKi = 5.6 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44397283 139452 0 None -181 3 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL187659 139452 0 None -181 3 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 591 11 3 5 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434692 179383 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235176 179383 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 651 13 3 5 8.3 COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434847 179815 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236442 179815 0 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 11 4 2 7.0 N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434778 180572 0 None -27 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -27 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434765 317297 0 None -20 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL413982 317297 0 None -20 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 643 11 3 3 9.1 NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
137641157 312974 0 None -223 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137655905 312974 0 None -223 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074074 312974 0 None -223 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 312974 0 None -223 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
16007263 161259 0 None -41 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 161259 0 None -41 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
24848995 236780 0 None 11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 236780 0 None 11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL263878 486112 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 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 40216 0 None -181 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
CHEMBL122773 40216 0 None -181 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 794 10 9 7 1.3 CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
24180646 294869 0 None -338 7 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 294869 0 None -338 7 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
11237444 255419 0 None -457 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 255419 0 None -457 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
44397304 254793 0 None -199 4 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365465 254793 0 None -199 4 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 579 11 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434764 179419 0 None -11 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235358 179419 0 None -11 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 551 10 2 2 7.8 NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434884 179470 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235617 179470 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434689 180032 0 None -19 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236649 180032 0 None -19 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 431 14 2 2 5.9 NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10291370 292679 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391823 292679 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 7 2 2 4.1 C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434762 309160 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 309160 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44409140 278520 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL383256 278520 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
44401386 141774 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL193409 141774 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 593 12 6 4 3.6 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.03.120
137636677 312024 0 None -50 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4063111 312024 0 None -50 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137636965 312140 0 None -23 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4064433 312140 0 None -23 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44409337 335012 0 None -114 3 Human 4.6 pKi = 4.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL444883 335012 0 None -114 3 Human 4.6 pKi = 4.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL2370553 477661 0 None -16 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1520 26 17 20 -2.1 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 142367 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL194011 142367 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
11341046 139167 0 None -95 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
CHEMBL186339 139167 0 None -95 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 501 7 4 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1 10.1021/jm0400496
44562440 352942 0 None -38 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL471340 352942 0 None -38 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 534 10 3 5 3.7 CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1 10.1016/j.bmcl.2008.07.076
44434880 179469 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235616 179469 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434647 180419 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
CHEMBL237483 180419 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.3 NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3 10.1016/j.bmc.2007.06.003
44434767 180564 0 None -17 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237689 180564 0 None -17 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 616 11 3 4 8.2 N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44434868 296232 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL394669 296232 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 635 11 5 4 6.7 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434762 309160 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL397550 309160 0 None -13 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 579 11 2 4 7.7 COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44434768 310745 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL399811 310745 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 553 9 2 2 8.3 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
11308054 271089 0 None -8 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL371365 271089 0 None -8 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 618 13 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413914 270550 0 None -40 3 Human 7.6 pKi = 7.6 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 270550 0 None -40 3 Human 7.6 pKi = 7.6 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
168289457 374445 0 None -16 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 374445 0 None -16 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44456222 198224 0 None -223 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 198224 0 None -223 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
44323033 216794 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 216794 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44434694 179460 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
CHEMBL235589 179460 0 None -12 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 665 14 3 5 8.7 CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC 10.1016/j.bmc.2007.06.003
44434761 180024 0 None -3 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236626 180024 0 None -3 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 625 11 3 3 8.9 NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434592 180345 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237315 180345 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434682 295286 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393919 295286 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 451 13 2 2 6.1 NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
172441036 387559 0 None -1862 3 Human 6.6 pKi = 6.6 Binding
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 387559 0 None -1862 3 Human 6.6 pKi = 6.6 Binding
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 352611 0 None -42 3 Human 4.6 pKi = 4.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL468252 352611 0 None -42 3 Human 4.6 pKi = 4.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL5075712 478591 0 None -181 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1924 27 27 22 -2.2 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](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 158571 0 None -338 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 158571 0 None -338 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 158571 0 None -338 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 158571 0 None -338 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
23635237 182263 0 None -45 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
CHEMBL240364 182263 0 None -45 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1021/jm070806a
23635237 182263 0 None -45 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL240364 182263 0 None -45 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 498 9 2 4 4.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1 10.1016/j.bmc.2008.03.072
44401513 141424 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL192450 141424 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 612 13 5 6 2.5 N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44434581 331854 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL428903 331854 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 7 2 2 5.2 NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1 10.1016/j.bmc.2007.06.003
44434772 179456 0 None -21 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -21 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434683 180147 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL236847 180147 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 10 3 3 4.9 C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
44434769 180568 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237698 180568 0 None -16 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 659 11 3 3 9.6 NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434650 180727 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237910 180727 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 11 2 2 4.8 NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434651 180728 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237911 180728 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 495 13 3 3 6.1 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434654 180849 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238134 180849 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 10 2 2 5.4 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434863 294832 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393552 294832 0 None -10 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 417 9 2 2 5.3 NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
168282596 373981 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
CHEMBL5185132 373981 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2990 66 33 37 -3.8 CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/acs.jmedchem.2c00786
168281389 373997 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
CHEMBL5185405 373997 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2149 33 33 26 -5.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O 10.1021/acs.jmedchem.2c00793
44323233 216377 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL314401 216377 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 901 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44322986 215781 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 215781 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11249545 138497 0 None -478 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
CHEMBL184432 138497 0 None -478 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1 10.1021/jm0400496
11364326 138975 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 138975 0 None -134 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
24740653 179451 0 None -758 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL235556 179451 0 None -758 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 540 11 1 4 5.3 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
44265707 24483 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159701 24483 0 None -4 4 Human 4.6 pKi = 4.6 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 354 10 3 4 2.1 C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434759 179374 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235139 179374 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434688 180030 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236640 180030 0 None -8 4 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.4 NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168286369 374770 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5197030 374770 0 None -4 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2962 64 33 37 -4.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
137640703 313008 0 None -218 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4074479 313008 0 None -218 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25133209 347449 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 347449 0 None -56 3 Human 6.6 pKi = 6.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
25128748 373092 0 None -28 3 Human 5.6 pKi = 5.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 373092 0 None -28 3 Human 5.6 pKi = 5.6 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL50056 484368 1 None -41 3 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm060384p
11845630 270549 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 270549 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
11846673 161455 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 161455 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44347220 333129 0 None -112 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL434985 333129 0 None -112 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 861 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL268851 486276 0 None -33 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 1074 17 13 11 -0.1 CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O 10.1021/jm010165y
44347378 233448 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333262 233448 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 818 11 11 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434772 179456 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235582 179456 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 6.7 C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
9968756 180340 0 None -18 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL237299 180340 0 None -18 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 5 1 2 3.7 NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44434870 294836 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL393553 294836 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 449 8 2 2 5.9 NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44413842 270510 0 None -18 3 Human 4.5 pKi = 4.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 270510 0 None -18 3 Human 4.5 pKi = 4.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
168278271 374186 0 None -30 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 374186 0 None -30 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
6918276 39502 6 None -309 8 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL1221512 39502 6 None -309 8 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 559 18 4 9 1.7 CC[C@H](C)[C@@H](CO[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCS(C)(=O)=O)C(=O)OC(C)C)NC[C@@H](N)CS nan
CHEMBL415661 488409 0 None -21 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1372 25 18 17 -2.2 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
162643435 355513 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 355513 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 355513 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 355513 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44416057 162632 0 None -3 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 162632 0 None -3 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
162643518 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643518 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162673640 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776915 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4793346 355554 0 None -89 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1075 17 15 12 -1.3 CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
127036484 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
1323 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
92432 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL3735690 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL430239 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
127036484 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
1323 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
92432 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL3735690 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
CHEMBL430239 5482 39 None -48 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1024 17 13 11 -1.2 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)N)NC(=O)C 10.1021/acs.jmedchem.0c01620
168271899 373686 0 None -4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5180727 373686 0 None -4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3020 70 35 39 -5.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168271237 373575 0 None -10 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 373575 0 None -10 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44347379 233449 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333263 233449 0 None -5 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 750 9 9 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347106 234049 0 None -52 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL334309 234049 0 None -52 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 738 9 10 7 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434872 179423 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
CHEMBL235382 179423 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2007.06.003
44434634 180143 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236840 180143 0 None -16 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 1 5 6.5 COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2007.06.003
44434597 180442 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237530 180442 0 None -1 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 3.9 NCCCN(CCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL5080784 478889 0 None -75 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1887 23 23 21 -0.9 C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
25132866 337125 0 None -77 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
CHEMBL449131 337125 0 None -77 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1 10.1021/jm800525p
162672691 366554 0 None -57 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 366554 0 None -57 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162672691 366554 0 None -57 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 366554 0 None -57 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44562287 348306 0 None -331 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454900 348306 0 None -331 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 3.9 CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
25211670 348318 0 None -323 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL454916 348318 0 None -323 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 548 10 2 5 4.0 CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1 10.1016/j.bmcl.2008.07.076
44562460 372406 0 None -954 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
CHEMBL511826 372406 0 None -954 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 533 10 3 5 3.8 CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2008.07.076
44434690 180150 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434713 180425 0 None -14 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237502 180425 0 None -14 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 541 11 2 3 7.5 COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
44434855 180858 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -10 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434859 180862 0 None -17 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
CHEMBL238158 180862 0 None -17 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1 10.1016/j.bmc.2007.06.003
44265487 197689 0 None -1 4 Human 4.5 pKi = 4.5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269689 197689 0 None -1 4 Human 4.5 pKi = 4.5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 256 6 4 2 1.8 N=C(N)NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL412494 488226 0 None -125 3 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1339 25 18 17 -2.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
3198 461850 54 None -75 34 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
983 461850 54 None -75 34 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 461850 54 None -75 34 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
DB01127 461850 54 None -75 34 Human 4.5 pKi = 4.5 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
44577510 371922 0 None -199 3 Human 6.5 pKi = 6.5 Binding
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 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
44577523 371922 0 None -199 3 Human 6.5 pKi = 6.5 Binding
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 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 371922 0 None -199 3 Human 6.5 pKi = 6.5 Binding
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 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
CHEMBL508068 371922 0 None -199 3 Human 6.5 pKi = 6.5 Binding
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 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
CHEMBL5077811 478706 0 None -56 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1073 16 14 13 -1.6 CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
44320339 470908 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL85918 470908 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 410 9 1 2 6.0 NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
11845440 276030 0 None -26 3 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
CHEMBL377778 276030 0 None -26 3 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.7 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1 10.1021/jm060384p
24741624 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
44416197 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
44416349 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL215617 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL377231 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
CHEMBL425261 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R stably expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1016/j.bmcl.2006.06.075
24741624 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44416197 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44416349 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL215617 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL377231 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
CHEMBL425261 162554 0 None -22 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 525 8 1 4 5.9 COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1 10.1021/jm701137s
44397281 254515 0 None -288 3 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL365237 254515 0 None -288 3 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 587 12 3 5 4.0 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434633 180027 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236630 180027 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 423 11 2 2 5.3 NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25129107 347856 0 None -36 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 347856 0 None -36 3 Human 6.5 pKi = 6.5 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
137660993 315289 0 None -83 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 315289 0 None -83 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
11156852 137980 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL183434 137980 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uMDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor at 10 uM
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL408257 488005 0 None -77 3 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1174 21 16 15 -3.3 CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
24740419 294881 0 None -1318 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
CHEMBL393584 294881 0 None -1318 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 575 11 1 5 5.4 Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1 10.1021/jm701137s
44434690 180150 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -19 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434862 181073 0 None -20 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238368 181073 0 None -20 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 477 10 2 2 6.4 NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
10225762 292531 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL391707 292531 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 448 14 2 3 5.5 CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
44434601 293179 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL392223 293179 0 None -13 4 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 358 8 1 2 4.3 NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44265374 473451 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8825 473451 0 None -21 4 Human 4.5 pKi = 4.5 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 454 10 2 2 6.4 O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
44577060 371273 0 None -97 7 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 371273 0 None -97 7 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat MC3RBinding affinity at rat MC3R
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
172461915 389107 0 None -741 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO cells measured for 2 hrs by microbeta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO cells measured for 2 hrs by microbeta counter analysis
ChEMBL 464 4 1 8 3.0 COc1cc([C@@H](C)C(=O)N2CC[C@@]3(COc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1 10.1021/acs.jmedchem.2c02012
CHEMBL5432266 389107 0 None -741 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO cells measured for 2 hrs by microbeta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO cells measured for 2 hrs by microbeta counter analysis
ChEMBL 464 4 1 8 3.0 COc1cc([C@@H](C)C(=O)N2CC[C@@]3(COc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1 10.1021/acs.jmedchem.2c02012
CHEMBL2370966 485649 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1525 47 20 18 -3.0 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
10232787 277668 0 None -467 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380855 277668 0 None -467 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44415918 278765 0 None -17 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 278765 0 None -17 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
168295726 375436 0 None -56 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 375436 0 None -56 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44322923 473504 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 473504 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11375764 138978 0 None -1659 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 138978 0 None -1659 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
24882666 196080 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 385 10 5 3 1.7 N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
CHEMBL258295 196080 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 385 10 5 3 1.7 N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
44393450 251729 0 None 1 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362010 251729 0 None 1 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 518 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(c2ccccc2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44416060 162754 0 None -58 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 162754 0 None -58 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
10325955 330164 0 None -33 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 330164 0 None -33 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
11786860 138626 1 None -281 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185035 138626 1 None -281 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-3 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44434685 180028 0 None -17 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236638 180028 0 None -17 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 497 14 3 3 6.3 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434652 180729 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237912 180729 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 403 12 2 2 5.2 NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168289584 374841 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5198158 374841 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3108 98 37 41 -6.4 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
168294114 375225 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5204285 375225 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 4756 82 66 59 -5.7 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
44323211 216671 0 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL315397 216671 0 None None None Human 6.4 pKi = 6.4 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 768 7 9 8 -0.1 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44434666 179418 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235356 179418 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 434 9 1 3 5.8 NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1 10.1016/j.bmc.2007.06.003
44265672 24480 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159699 24480 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 442 10 5 3 3.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00089-6
44434754 181062 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 181062 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
10292084 295077 0 None -15 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL393755 295077 0 None -15 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 6 2 2 3.4 NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
25133208 336521 0 None -34 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 336521 0 None -34 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
168281969 374344 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 374344 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44322994 216651 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315258 216651 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 715 20 9 8 -1.0 COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44577063 371320 0 None -70 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL498150 371320 0 None -70 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 544 8 1 4 4.9 CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL5090670 479443 0 None -37 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1872 25 25 21 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44434616 179554 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236003 179554 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 10 2 2 4.8 CCC(c1ccccc1)N(CCCCN)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10159196 180567 0 None -6 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237694 180567 0 None -6 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 421 11 2 4 4.4 NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434635 333526 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL438334 333526 0 None -3 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 363 10 2 2 4.3 NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44409206 277473 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL380437 277473 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
11847312 161226 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 161226 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL5077095 478670 0 None -346 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1938 27 26 22 -1.9 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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090285 479421 0 None -138 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1862 25 26 22 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137646617 313441 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 313441 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46877881 465190 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL606990 465190 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 813 9 10 8 -0.3 N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
44400813 143317 0 None -134 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195308 143317 0 None -134 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 603 12 4 6 3.9 O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
9958649 252383 0 None -354 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
CHEMBL363730 252383 0 None -354 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 529 6 3 3 5.6 CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1 10.1021/jm0400496
156015336 351466 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
CHEMBL4639782 351466 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting
ChEMBL 3793 77 53 60 -15.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2 10.1021/acs.jmedchem.0c00485
44434657 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434658 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434714 295074 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL393753 295074 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 486 9 2 3 6.4 NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
137660671 315069 0 None -416 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 315069 0 None -416 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
168290510 374945 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5199932 374945 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1215 15 14 15 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5085972 477477 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL385556 487665 0 None -173 3 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1018 15 13 13 -1.9 CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
10077773 178140 4 None -204 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233135 178140 4 None -204 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 559 14 1 6 7.4 CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434850 180031 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL236645 180031 0 None -10 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 461 9 2 2 6.3 NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
11845276 161513 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 161513 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL5076315 478624 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1948 22 21 19 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](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
168281969 374344 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5190661 374344 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 3072 100 37 39 -7.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44434657 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44434658 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238341 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
CHEMBL238342 181061 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 10 2 3 3.9 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1 10.1016/j.bmc.2007.06.003
44415991 161964 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214770 161964 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1016/j.bmcl.2006.05.087
44415991 161964 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1021/jm800525p
CHEMBL214770 161964 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 519 9 3 5 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O 10.1021/jm800525p
44413831 159642 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL210008 159642 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
57817773 158569 0 None -245 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684623 158569 0 None -245 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929806 158569 0 None -245 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070249 158569 0 None -245 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1918 56 24 26 -3.6 CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44413930 270519 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 270519 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL433645 488592 0 None -104 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 781 9 10 8 -0.4 NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm010165y
23635235 331318 0 None -177 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
CHEMBL427860 331318 0 None -177 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1021/jm070806a
44410803 277461 0 None -398 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380365 277461 0 None -398 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 2 5 5.0 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1 10.1016/j.bmcl.2005.10.103
44434687 315333 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410179 315333 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 465 14 2 2 6.5 NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11846844 270569 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 270569 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
137653925 314477 0 None -18 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 314477 0 None -18 3 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25128751 347676 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 347676 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL438030 488691 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1551 47 21 18 -3.1 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
44434855 180858 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -10 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44434664 179417 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434665 179417 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235355 179417 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393383 179417 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 378 10 3 3 3.2 NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434684 293307 0 None -12 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392315 293307 0 None -12 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 391 12 2 2 5.0 NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25133207 347061 0 None -16 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
CHEMBL451694 347061 0 None -16 3 Human 6.4 pKi = 6.4 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 601 11 3 5 2.7 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1 10.1021/jm800525p
172456996 388642 0 None -56 3 Human 6.4 pKi = 6.4 Binding
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 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
172468229 388642 0 None -56 3 Human 6.4 pKi = 6.4 Binding
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 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 388642 0 None -56 3 Human 6.4 pKi = 6.4 Binding
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 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 388642 0 None -56 3 Human 6.4 pKi = 6.4 Binding
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 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
11845438 275020 0 None -10 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL375775 275020 0 None -10 3 Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 661 12 6 6 2.4 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44323034 473488 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 473488 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL91957 489409 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 817 20 10 8 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10257541 254315 0 None -269 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL365039 254315 0 None -269 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434851 180737 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
CHEMBL237930 180737 0 None -16 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 10 2 2 5.7 NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2007.06.003
10155513 298185 0 None -4 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396303 298185 0 None -4 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 8 2 2 4.0 C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL2070242 485053 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1510 32 22 20 -6.9 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44400810 252105 0 None -316 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 11 3 5 5.4 CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363190 252105 0 None -316 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 11 3 5 5.4 CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL2070373 477531 0 None -57 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2004 60 24 26 -1.2 CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44434562 179557 0 None -562 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236014 179557 0 None -562 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 551 10 3 5 3.9 CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmc.2007.05.026
44577094 352558 0 None -134 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL467588 352558 0 None -134 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 546 10 1 4 5.3 CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
10864861 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
10886436 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
10952071 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
1338 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
9938402 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL140108 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL334457 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL339053 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
CHEMBL342954 8293 40 None -75 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm0311285
44432964 178325 0 None -1148 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL233372 178325 0 None -1148 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 558 14 0 5 7.2 CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44453903 311386 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 387 9 2 5 2.7 N[C@H](Cc1ccc(F)cc1)C(=O)NCCC(Cn1cncn1)C1CCCCC1 10.1016/j.bmcl.2007.11.109
CHEMBL403722 311386 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 387 9 2 5 2.7 N[C@H](Cc1ccc(F)cc1)C(=O)NCCC(Cn1cncn1)C1CCCCC1 10.1016/j.bmcl.2007.11.109
44434865 179608 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL236226 179608 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 589 10 4 3 6.5 NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434690 180733 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237920 180733 0 None -14 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434849 293552 0 None -23 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
CHEMBL392521 293552 0 None -23 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 411 9 2 2 5.2 NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1 10.1016/j.bmc.2007.06.003
44434614 298226 1 None -2 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396341 298226 1 None -2 4 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.9 NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265472 473327 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL8742 473327 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 245 6 5 2 1.1 N=C(N)NCCCNCc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
51346771 121016 0 None -13 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL1682208 121016 0 None -13 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC3 receptor expressed in BHK cells
ChEMBL 671 10 2 9 3.3 COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3 10.1016/j.bmcl.2011.01.011
CHEMBL214332 485136 29 None -30 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1664 50 23 22 -4.5 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
44410802 277672 0 None -263 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL380858 277672 0 None -263 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 633 12 1 5 5.3 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1 10.1016/j.bmcl.2005.10.103
44434686 293308 0 None -15 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
CHEMBL392316 293308 0 None -15 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 407 11 3 3 4.7 CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1 10.1016/j.bmc.2007.06.003
44434698 335567 0 None -16 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
CHEMBL445669 335567 0 None -16 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 649 12 3 5 8.1 COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1 10.1016/j.bmc.2007.06.003
44416122 161587 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213284 161587 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
44409104 158179 0 None -36 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL206033 158179 0 None -36 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
44323234 40519 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347221 40519 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL124169 40519 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432377 40519 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 903 11 12 9 0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44416135 161642 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 161642 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416135 161642 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
CHEMBL213566 161642 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
44434663 179373 0 None -23 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235138 179373 0 None -23 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 483 13 3 3 5.9 NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434637 180252 0 None -5 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237052 180252 0 None -5 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 377 11 2 2 4.3 NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
25129108 346831 0 None -33 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL450236 346831 0 None -33 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 629 11 3 5 3.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1 10.1021/jm800525p
CHEMBL5091236 479464 0 None -602 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1980 28 24 22 -1.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL441760 488836 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1555 30 20 19 -2.5 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC(C)(C)[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44265751 215782 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL313379 215782 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44434611 179473 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
CHEMBL235627 179473 0 None -7 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 373 6 2 2 3.9 NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1 10.1016/j.bmc.2007.06.003
44401392 24590 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
46905544 24590 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161791 24590 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL191975 24590 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44577060 371273 0 None -141 7 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 371273 0 None -141 7 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
44434580 298539 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 335 8 2 2 3.5 NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL396598 298539 0 None -2 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 335 8 2 2 3.5 NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168281421 374031 0 None -89 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 374031 0 None -89 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168284256 374020 0 None -14 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 374020 0 None -14 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL409636 488073 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1604 35 21 18 -2.5 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
44322868 215692 0 None 4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL313279 215692 0 None 4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 917 11 12 9 0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL253364 486024 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 932 11 13 10 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](N)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm070461w
44413931 159593 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 159593 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5087839 479291 0 None -69 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1864 23 22 21 -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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
71458055 160518 0 None 7 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
CHEMBL2113133 160518 0 None 7 4 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 6 2 5 3.7 CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21 10.1016/j.bmcl.2005.07.035
16038315 276113 0 None -741 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
CHEMBL378046 276113 0 None -741 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 612 13 3 7 3.5 COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1 10.1016/j.bmcl.2006.04.069
44434839 179512 0 None -4 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235802 179512 0 None -4 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10157774 180145 0 None -33 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236842 180145 0 None -33 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 9 2 2 5.0 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434861 181072 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238367 181072 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 389 7 2 2 4.8 N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
44413881 274990 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 274990 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
44265751 215782 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL313379 215782 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 412 12 7 4 0.3 N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL5091245 479465 0 None -120 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1911 26 24 22 -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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
10025669 197698 0 None -79 4 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
CHEMBL269776 197698 0 None -79 4 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1021/jm020945m
168276294 373595 0 None -23 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179373 373595 0 None -23 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 3264 55 36 40 1.5 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5087859 479294 0 None -741 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1966 27 24 22 -1.2 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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44434570 180608 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237719 180608 0 None -3 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 347 8 2 2 3.6 NCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434754 181062 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238345 181062 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 557 11 3 4 7.2 COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1 10.1016/j.bmc.2007.06.003
172446133 387855 0 None -354 3 Human 6.3 pKi = 6.3 Binding
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 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
172457809 387855 0 None -354 3 Human 6.3 pKi = 6.3 Binding
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 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 387855 0 None -354 3 Human 6.3 pKi = 6.3 Binding
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 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 387855 0 None -354 3 Human 6.3 pKi = 6.3 Binding
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 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
44393417 196927 0 None -13 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL263182 196927 0 None -13 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434770 179420 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL235359 179420 0 None -29 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 521 9 2 2 7.3 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434857 310475 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398980 310475 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 475 13 2 4 3.9 NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
71461662 160606 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL2113280 160606 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 442 9 4 3 3.2 NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12 10.1016/s0960-894x(02)00088-4
44401607 271090 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 635 15 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL371366 271090 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 635 15 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1 10.1016/j.bmcl.2005.03.120
44413828 270545 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 270545 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
10408 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
5329 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
CHEMBL2070241 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
DB11653 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
44265711 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44265749 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
23653113 179511 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235798 179511 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 427 9 4 2 4.2 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
137659790 315167 0 None -102 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 315167 0 None -102 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44347840 317432 0 None -17 3 Human 7.3 pKi = 7.3 Binding
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
91932630 317432 0 None -17 3 Human 7.3 pKi = 7.3 Binding
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
CHEMBL415333 317432 0 None -17 3 Human 7.3 pKi = 7.3 Binding
Inhibitory activity against human Melanocortin 3 receptor was determinedInhibitory activity against human Melanocortin 3 receptor was determined
ChEMBL 1590 33 17 23 -2.2 CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm030111j
44322788 313283 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 313283 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44322957 473196 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 473196 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44432966 293011 0 None -562 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
CHEMBL392092 293011 0 None -562 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 3 receptor expressed in CHOK1 cells
ChEMBL 560 14 0 6 6.7 COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.06.010
44434649 292526 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 453 12 2 2 6.4 NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391705 292526 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 453 12 2 2 6.4 NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434653 292529 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL391706 292529 0 None -6 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 437 12 2 2 5.7 NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434787 295472 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394075 295472 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 729 13 3 5 9.1 COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL264352 486129 0 None -104 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1338 25 18 17 -2.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
44434696 295874 0 None -54 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394394 295874 0 None -54 4 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 609 11 3 3 8.4 NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44409339 156664 0 None -1479 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL203252 156664 0 None -1479 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
44347119 233438 0 None -151 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL333178 233438 0 None -151 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 752 9 10 7 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL267900 486245 0 None -144 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1174 21 16 15 -3.3 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
44400934 142856 0 None -281 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194987 142856 0 None -281 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 10 2 5 4.9 CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44393418 311635 0 None -5 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL405150 311635 0 None -5 4 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 589 8 2 7 3.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44265711 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44265749 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9138 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL9274 473921 0 None -4 4 Human 4.3 pKi = 4.3 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 343 6 3 2 3.5 NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
10025669 197698 0 None -79 4 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269776 197698 0 None -79 4 Human 4.3 pKi = 4.3 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 429 11 5 4 3.0 NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
44400660 142962 0 None -239 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL195071 142962 0 None -239 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 558 10 2 5 4.8 CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44577090 352577 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL467771 352577 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 502 9 2 4 4.0 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
44434598 180645 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237743 180645 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 349 9 2 2 3.5 NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434867 179381 0 None -26 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
CHEMBL235162 179381 0 None -26 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1 10.1016/j.bmc.2007.06.003
44434790 181065 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238353 181065 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 399 7 4 2 3.4 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265309 470487 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8201 470487 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 214 5 2 2 2.3 NCCCNCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
44400814 142864 0 None -446 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 627 11 3 5 5.9 O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194990 142864 0 None -446 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 627 11 3 5 5.9 O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44322987 197060 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 197060 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10158674 294607 0 None -7 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393359 294607 0 None -7 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 10 2 2 5.4 NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44265347 197291 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL266305 197291 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 426 10 4 4 3.3 NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1 10.1016/s0960-894x(02)00088-4
23635235 331318 0 None -177 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 331318 0 None -177 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
44347110 233133 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL332762 233133 0 None -6 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 681 9 9 7 0.6 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347081 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347082 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44347330 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL420727 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL432407 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
CHEMBL436169 328872 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 3 (hMC3R) (concentration of the peptide at 50% specific binding)
ChEMBL 766 9 10 7 0.9 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm010165y
44434864 181074 0 None -21 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL238369 181074 0 None -21 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1 10.1016/j.bmc.2007.06.003
2852098 470306 11 None -4 3 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL8045 470306 11 None -4 3 Human 4.2 pKi = 4.2 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 300 5 2 1 4.7 c1ccc2cc(CNCCc3c[nH]c4ccccc34)ccc2c1 10.1016/s0960-894x(02)00088-4
CHEMBL439128 488768 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1640 35 21 20 -2.6 CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL412523 488229 0 None -22 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1388 25 18 17 -1.7 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
44434639 294844 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393557 294844 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 405 13 2 2 5.1 NCCCCCN(CCCc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44416014 161475 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212855 161475 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
44409338 333396 0 None -1230 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL437132 333396 0 None -1230 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to MC3 receptorBinding affinity to MC3 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
44434778 180572 0 None -27 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237702 180572 0 None -27 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 544 9 1 3 7.8 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1 10.1016/j.bmc.2007.06.003
44434853 197517 0 None -5 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 8 2 2 5.3 N[C@@H]1CCCC[C@H]1N(C/C=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL268395 197517 0 None -5 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 415 8 2 2 5.3 N[C@@H]1CCCC[C@H]1N(C/C=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
11215758 138373 0 None -131 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
CHEMBL183799 138373 0 None -131 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for human melanocortin 3 receptorBinding affinity for human melanocortin 3 receptor
ChEMBL 624 9 3 6 5.0 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2004.10.096
44322924 216756 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316038 216756 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 701 19 11 8 -1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
10177247 180344 0 None -5 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237314 180344 0 None -5 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 371 7 2 2 4.2 NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
10200110 180562 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237687 180562 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 385 8 2 2 4.6 NCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434605 296194 0 None -9 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
CHEMBL394647 296194 0 None -9 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 356 10 1 3 4.4 C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1 10.1016/j.bmc.2007.06.003
168277258 373793 0 None -109 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5182345 373793 0 None -109 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1243 15 14 15 -0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
6918814 255024 0 None -354 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL365597 255024 0 None -354 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44433264 180191 0 None -144 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236940 180191 0 None -144 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 598 8 1 4 5.9 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
6918814 255024 0 None -354 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
CHEMBL365597 255024 0 None -354 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC3receptor expressed in HEK293 cells
ChEMBL 587 12 3 6 4.1 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1021/jm049278i
44265639 24478 0 None -5 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL1159697 24478 0 None -5 4 Human 5.2 pKi = 5.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 439 9 4 3 4.1 NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
44434854 180857 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238153 180857 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 573 10 2 2 8.6 CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
44323031 332809 0 None -10 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 332809 0 None -10 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44397028 252079 0 None -85 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
CHEMBL363019 252079 0 None -85 4 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 631 12 3 6 3.6 COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1 10.1016/j.bmcl.2005.05.017
44392514 251924 0 None -7 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL362670 251924 0 None -7 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 7 2 7 3.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
44434794 179378 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235147 179378 0 None -4 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 413 8 4 2 3.8 N=C(N)NCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434600 295284 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL393918 295284 0 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 361 9 2 2 4.0 NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44434771 295470 0 None -30 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL394073 295470 0 None -30 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 627 11 3 3 8.6 NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434572 331407 0 None -11 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 9 2 2 4.6 NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL428022 331407 0 None -11 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 9 2 2 4.6 NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44401367 317252 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL413565 317252 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44323032 473558 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 473558 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
172469229 389387 0 None -831 3 Human 6.2 pKi = 6.2 Binding
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 873 11 11 10 0.4 N#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
CHEMBL5438253 389387 0 None -831 3 Human 6.2 pKi = 6.2 Binding
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 873 11 11 10 0.4 N#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
44434855 180858 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
CHEMBL238154 180858 0 None -10 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 513 9 2 2 7.5 CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N 10.1016/j.bmc.2007.06.003
57817730 158567 0 None -338 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684622 158567 0 None -338 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929805 158567 0 None -338 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070247 158567 0 None -338 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
44400935 143094 0 None -446 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
CHEMBL195110 143094 0 None -446 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 613 10 2 5 5.5 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1 10.1016/j.bmcl.2005.03.053
44434632 293019 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL392096 293019 0 None -8 4 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 10 2 2 4.4 NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL410168 488101 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1527 30 20 19 -3.3 CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44393421 241661 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL361052 241661 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 508 6 2 4 3.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
70682904 159440 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
70684954 159440 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL2092821 159440 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
CHEMBL2093089 159440 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 383 5 2 2 4.6 O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12 10.1016/s0960-894x(02)00089-6
9924916 179867 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL236447 179867 0 None -3 3 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 357 6 2 2 3.9 NCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
168279695 374206 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 374206 0 None -2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL437050 484343 3 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.
ChEMBL 1570 47 21 19 -2.9 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/jm030119t
44401581 140901 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL191794 140901 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 602 13 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44416106 278671 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 278671 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44323020 333622 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL439188 333622 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 951 11 12 9 1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL2373515 485964 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1862 40 24 25 -5.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
172456996 388642 0 None -56 3 Human 8.1 pKi = 8.1 Binding
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 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
172468229 388642 0 None -56 3 Human 8.1 pKi = 8.1 Binding
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 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 388642 0 None -56 3 Human 8.1 pKi = 8.1 Binding
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 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 388642 0 None -56 3 Human 8.1 pKi = 8.1 Binding
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 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
11226756 238670 0 None -114 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349850 238670 0 None -114 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 559 8 2 5 3.5 CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
6918857 276064 0 None -239 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
CHEMBL377961 276064 0 None -239 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cellDisplacement of [125I]NDP-alpha-MSH from cloned human MC3R expressed in HEK293 cell
ChEMBL 619 11 2 5 4.4 CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.10.103
44413880 159529 0 None -46 3 Human 6.2 pKi = 6.2 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 159529 0 None -46 3 Human 6.2 pKi = 6.2 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
44401587 24592 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 611 15 6 5 2.6 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161794 24592 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 611 15 6 5 2.6 N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL5094215 479637 0 None -60 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1825 23 21 21 -0.3 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](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2070374 477532 2 None -123 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 2091 63 26 29 -4.9 CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
23635236 182406 0 None -123 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
CHEMBL240780 182406 0 None -123 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3RDisplacement of [125I]NDP-MSH from human MC3R
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1021/jm070806a
23635236 182406 0 None -123 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
CHEMBL240780 182406 0 None -123 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 512 10 2 4 4.6 CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmc.2008.03.072
24180592 197336 0 None -208 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 197336 0 None -208 5 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44397198 139052 0 None -93 3 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
CHEMBL185862 139052 0 None -93 3 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells Inhibition of [125I]-NDP-MSH (radioligand) binding to the human MC3R stably expressed in HEK293 cells
ChEMBL 601 11 3 5 3.6 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.05.017
44434690 180150 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236861 180150 0 None -19 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 545 10 2 2 8.1 NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44413832 159643 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL210009 159643 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
11845804 161039 0 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL211419 161039 0 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
25133907 350684 0 None -9 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 350684 0 None -9 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
10864861 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
10886436 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
10952071 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
1338 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
9938402 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
CHEMBL140108 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
CHEMBL334457 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
CHEMBL339053 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
CHEMBL342954 8293 40 None -75 4 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.03.120
10178845 180742 0 None -7 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL237937 180742 0 None -7 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 395 8 2 3 3.8 NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
172447505 388250 0 None -3162 3 Human 6.1 pKi = 6.1 Binding
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 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 388250 0 None -3162 3 Human 6.1 pKi = 6.1 Binding
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 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
44413969 161687 0 None -21 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 161687 0 None -21 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44415912 276552 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 276552 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MC3RBinding affinity to human MC3R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
24180646 294869 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 294869 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
24180646 294869 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 294869 0 None -1071 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
44434821 180856 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL238149 180856 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 441 10 4 2 4.5 N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
137647538 313847 0 None -1318 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 313847 0 None -1318 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
25131478 334080 0 None -53 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
CHEMBL443396 334080 0 None -53 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
44443035 310466 0 None -1258 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
CHEMBL398929 310466 0 None -1258 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to MC3RBinding affinity to MC3R
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
44322795 473859 0 None -13 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL91041 473859 0 None -13 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cellsBinding affinity for human Melanocortin-3 receptor (hMC3R) expressed in HEK293 cells
ChEMBL 853 11 12 9 -0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm020021z
CHEMBL50056 484368 1 None -41 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 685 18 9 7 -0.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44401392 24590 0 None 2 2 Human 5.1 pKi = 5.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
46905544 24590 0 None 2 2 Human 5.1 pKi = 5.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL1161791 24590 0 None 2 2 Human 5.1 pKi = 5.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL191975 24590 0 None 2 2 Human 5.1 pKi = 5.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 641 14 6 5 2.6 CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44434702 296193 0 None -26 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
CHEMBL394646 296193 0 None -26 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 605 11 3 3 8.6 Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1 10.1016/j.bmc.2007.06.003
44434856 310442 0 None -16 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
CHEMBL398777 310442 0 None -16 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 535 14 2 4 5.0 NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2007.06.003
172446133 387855 0 None -354 3 Human 7.1 pKi = 7.1 Binding
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 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
172457809 387855 0 None -354 3 Human 7.1 pKi = 7.1 Binding
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 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 387855 0 None -354 3 Human 7.1 pKi = 7.1 Binding
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 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 387855 0 None -354 3 Human 7.1 pKi = 7.1 Binding
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 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
44400864 252355 0 None -467 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL363576 252355 0 None -467 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 587 11 3 5 5.0 CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
6918844 333287 0 None -245 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
CHEMBL436122 333287 0 None -245 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 606 12 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF 10.1016/j.bmcl.2005.03.053
44265496 197371 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
CHEMBL267020 197371 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 3 receptor, expressed as negative log of the Ki value
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1021/jm020945m
70688853 158568 0 None -23 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070248 158568 0 None -23 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
57646437 158566 0 None -74 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684621 158566 0 None -74 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929804 158566 0 None -74 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070246 158566 0 None -74 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
162669632 356382 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 356382 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162669632 356382 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 356382 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
25129453 336297 0 None -14 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 336297 0 None -14 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
44400932 142547 0 None -173 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 588 11 2 6 5.4 CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL194393 142547 0 None -173 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 588 11 2 6 5.4 CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
16007285 162566 0 None -61 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
CHEMBL215659 162566 0 None -61 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC3R expressed in HEK293 cells
ChEMBL 586 10 2 4 5.8 CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2006.05.088
44434709 180604 0 None -21 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237714 180604 0 None -21 4 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 563 9 2 2 7.7 NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44400778 273331 0 None -162 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 574 10 2 6 5.0 COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL373099 273331 0 None -162 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 574 10 2 6 5.0 COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434785 295471 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL394074 295471 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 623 11 2 4 7.8 COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
44413968 161686 0 None -426 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 161686 0 None -426 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
172468874 389400 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
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 863 11 12 10 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5438629 389400 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
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 863 11 12 10 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.2c01587
24740655 179943 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
CHEMBL236521 179943 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human MC3RBinding affinity at human MC3R
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1016/j.bmcl.2007.07.097
24740655 179943 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
CHEMBL236521 179943 0 None -1380 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NDPMSH from human MC3R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC3R expressed in HEK293 cells
ChEMBL 643 12 1 5 5.3 Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1 10.1021/jm701137s
58777892 160534 0 None -117 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
CHEMBL2113149 160534 0 None -117 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 3 receptor
ChEMBL 599 7 2 5 3.9 CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1 10.1016/j.bmcl.2005.07.035
44265681 24482 0 None -28 2 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 369 7 4 4 0.6 NC(N)=NCCCNC(=O)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
CHEMBL1159700 24482 0 None -28 2 Human 4.1 pKi = 4.1 Binding
Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 3 receptor
ChEMBL 369 7 4 4 0.6 NC(N)=NCCCNC(=O)[C@@H]1C[C@H](O)CN1Cc1ccc2ccccc2c1 10.1016/s0960-894x(02)00089-6
44413879 276248 0 None -64 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 276248 0 None -64 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
25132526 372096 0 None -43 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
CHEMBL507876 372096 0 None -43 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 602 10 2 4 4.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C 10.1021/jm800525p
168279695 374206 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5188196 374206 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 66 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44400777 140941 0 None -295 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 630 13 2 7 4.7 COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL192090 140941 0 None -295 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 630 13 2 7 4.7 COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434763 297990 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL396111 297990 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 685 13 3 5 9.0 COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
168285904 374731 0 None -169 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 374731 0 None -169 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44413830 159533 0 None -8 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209622 159533 0 None -8 3 Human 6.1 pKi = 6.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL5083551 479049 0 None -93 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1853 23 23 21 -1.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
11845272 161812 0 None -8 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 161812 0 None -8 3 Human 7.1 pKi = 7.1 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44400809 140673 0 None -407 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 599 11 3 5 5.1 O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL191701 140673 0 None -407 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 599 11 3 5 5.1 O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
2163781 197684 7 None -4 3 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
CHEMBL269653 197684 7 None -4 3 Human 4.1 pKi = 4.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 289 5 3 1 4.0 c1ccc2c(CCNCc3c[nH]c4ccccc34)c[nH]c2c1 10.1016/s0960-894x(02)00088-4
44401553 142073 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 648 14 4 5 3.7 COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.03.120
CHEMBL193715 142073 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 648 14 4 5 3.7 COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.03.120
25133903 335109 0 None -15 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
CHEMBL445009 335109 0 None -15 3 Human 5.1 pKi = 5.1 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
44392535 136603 0 None -16 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
CHEMBL180937 136603 0 None -16 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Melanocortin 3 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 3 receptor using [125I]NDP-MSH
ChEMBL 575 8 2 7 2.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1 10.1021/jm0311285
9808720 136553 0 None -39 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
9960253 136553 0 None -39 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL180892 136553 0 None -39 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 136553 0 None -39 4 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cellsBinding affinity towards human Melanocortin 3 receptor (MC3R) using [125I]NDP-alpha-MSH as a radioligand in membranes of HEK 293 cells
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
168295173 375344 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 375344 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL89270 489403 0 None -17 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)Binding affinity towards human Melanocortin 3 receptor (hMC3R)
ChEMBL 643 17 9 7 -0.8 NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1016/s0960-894x(03)00552-3
CHEMBL5077144 478676 0 None -575 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1823 25 25 22 -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)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5092761 479551 0 None -1258 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1987 26 22 22 0.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL428326 488513 0 None -17 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1958 57 25 26 -6.9 CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
168295173 375344 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5206293 375344 0 None -2 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
44401285 273115 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 636 13 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
CHEMBL372966 273115 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity towards human Melanocortin 3 ReceptorInhibitory activity towards human Melanocortin 3 Receptor
ChEMBL 636 13 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1 10.1016/j.bmcl.2005.03.120
44265496 197371 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
CHEMBL267020 197371 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Tested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 3 receptor by using radioligand binding assay
ChEMBL 453 9 3 3 3.9 NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12 10.1016/s0960-894x(02)00088-4
10134057 179516 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
CHEMBL235815 179516 0 None -5 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 375 8 2 3 3.6 C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2007.06.003
44453902 195802 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 391 10 5 3 2.4 N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
CHEMBL257040 195802 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells
ChEMBL 391 10 5 3 2.4 N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2007.11.109
168274920 373357 0 None -83 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 373357 0 None -83 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44434715 332279 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 593 10 2 3 7.8 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
CHEMBL429983 332279 0 None -3 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 593 10 2 3 7.8 COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br 10.1016/j.bmc.2007.06.003
44434781 180732 0 None -15 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL237919 180732 0 None -15 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 485 9 2 2 7.0 NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
44434758 179553 0 None -100 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
CHEMBL236002 179553 0 None -100 4 Human 4.0 pKi = 4.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 755 14 3 5 9.6 COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC 10.1016/j.bmc.2007.06.003
25132524 350718 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 350718 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC3R expressed in HEK293 cells
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44400662 253183 0 None -478 2 Human 6.0 pKi = 6.0 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 13 3 6 4.5 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL364463 253183 0 None -478 2 Human 6.0 pKi = 6.0 Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
ChEMBL 601 13 3 6 4.5 NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1 10.1016/j.bmcl.2005.03.053
44434568 180033 0 None -213 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL236650 180033 0 None -213 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]NDP-MSH from MC3R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC3R receptor in HEK293 cells
ChEMBL 613 8 2 5 4.8 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434843 179559 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL236020 179559 0 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 587 11 4 2 7.6 N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
168285313 374465 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
CHEMBL5192562 374465 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells by Topcount beta counter analysis
ChEMBL 2967 62 33 39 -5.5 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O 10.1021/acs.jmedchem.2c00786
172468014 388892 0 None -660 3 Human 7.0 pKi = 7.0 Binding
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 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 388892 0 None -660 3 Human 7.0 pKi = 7.0 Binding
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 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
CHEMBL412495 488227 0 None -79 3 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cellsInhibition of [125I]-NDP-alpha-MSH binding to melanocortin-3 receptor expressed in HEK293 cells
ChEMBL 1310 25 17 17 -1.8 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
168272615 373477 0 None -87 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 373477 0 None -87 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44434858 332043 0 None -9 3 Human 4.0 pKi = 4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
CHEMBL429269 332043 0 None -9 3 Human 4.0 pKi = 4 Binding
Displacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC3 receptor expressed in Sf9 cells
ChEMBL 529 9 4 3 5.4 N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmc.2007.06.003
11292 891 0 None None None Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
70669253 891 0 None None None Human 6.4 pKd = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 5 2 5 1.7 NC(=N/N=C\C=C\c1cccn1c1ccccc1[N+](=O)[O-])N None
1326 7717 0 None 1 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15840392
1321 3973 0 None -15 3 Human 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10657491
1328 3975 0 None -15 4 Human 8.3 pKd None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9832440
1333 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
44134812 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
57339641 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01189 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01193 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01194 3608 0 None None None Human 8.5 pKd None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
3198 461850 54 None -75 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
983 461850 54 None -75 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 461850 54 None -75 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
DB01127 461850 54 None -75 34 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2726 1895 54 None -158 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 1895 54 None -158 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 1895 54 None -158 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 1895 54 None -158 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 1895 54 None -158 48 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1016 8173 46 None -56 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 8173 46 None -56 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 8173 46 None -56 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 8173 46 None -56 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 8173 46 None -56 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1800 473856 65 None -54 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4189 473856 65 None -54 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 473856 65 None -54 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
DB01110 473856 65 None -54 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2247 1042 63 None -109 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 1042 63 None -109 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 1042 63 None -109 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 1042 63 None -109 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 1042 63 None -109 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
176 823 54 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 823 54 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 823 54 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 823 54 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 823 54 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
134611880 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
16132265 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
3633 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
4931 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
CHEMBL1201610 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
DB01285 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
P01189 570 0 None -5 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N None
11993702 7304 0 None -4 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
5416 7304 0 None -4 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
9272 7304 0 None -4 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
DB11700 7304 0 None -4 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N None
122194229 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
1324 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
16197727 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
4836 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL3629347 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
CHEMBL441738 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
DB04931 621 23 None -4 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO None
10408 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
5329 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
9941379 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
CHEMBL2070241 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
DB11653 1486 31 None -26 4 Human 7.3 pKi = 7.3 Binding
Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.Inhibition of <sup>125</sup>I-NDP-&alpha;MSH binding to membranes from BHK570 cells stably expressing human MC<sub>3</sub> receptor.
Guide to Pharmacology 1025 17 13 11 -0.6 CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 22335602
134611880 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
16132265 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
3633 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
4931 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
CHEMBL1201610 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
DB01285 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
P01189 570 0 None -5 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 4538 145 60 61 -15.8 NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccccc1)CCC(=O)O)CC(C)C)Cc1ccccc1)C)CCC(=O)O)C)CO)CCC(=O)O)CC(=O)O)CCC(=O)O)C)CC(=O)N)Cc1ccc(cc1)O)C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)N)Cc1ccc(cc1)O)CO)CCSC)CCC(=O)O)Cc1nc[nH]c1)Cc1ccccc1)CCCN=C(N)N)CCCCN)CCCCN)CCCCN)CCCN=C(N)N)CCCN=C(N)N 7774675
11993702 7304 0 None -4 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
5416 7304 0 None -4 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
9272 7304 0 None -4 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
DB11700 7304 0 None -4 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1116 18 15 14 -3.2 NC(=NCCC[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC1=O)C)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)N)NC(=O)C)N 19646498
127035019 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
127035019 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 12007532
127035019 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 7658432
1325 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
1325 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 12007532
1325 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 7658432
9898183 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
9898183 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 12007532
9898183 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 7658432
CHEMBL3422426 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
CHEMBL3422426 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 12007532
CHEMBL3422426 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 7658432
CHEMBL3735607 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10657491
CHEMBL3735607 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 12007532
CHEMBL3735607 7320 11 None -5 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 7658432
127035019 7320 11 None -12 4 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10493100
1325 7320 11 None -12 4 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10493100
9898183 7320 11 None -12 4 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10493100
CHEMBL3422426 7320 11 None -12 4 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10493100
CHEMBL3735607 7320 11 None -12 4 Rat 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1074 17 14 11 0.1 C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@@H](NC([C@H](CCCC)NC(C)=O)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC3=O 10493100
1320 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
1320 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
16162729 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
16162729 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
P01189 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01189 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
P01193 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01193 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
P01194 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10358030
P01194 757 0 None 3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10493100
127036484 5482 39 None -48 4 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 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)N)NC(=O)C 10493100
1323 5482 39 None -48 4 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 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)N)NC(=O)C 10493100
92432 5482 39 None -48 4 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 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)N)NC(=O)C 10493100
CHEMBL3735690 5482 39 None -48 4 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 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)N)NC(=O)C 10493100
CHEMBL430239 5482 39 None -48 4 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1024 17 13 11 -1.2 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)N)NC(=O)C 10493100
122194229 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
1324 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
16197727 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
4836 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
CHEMBL3629347 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
CHEMBL441738 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100
DB04931 621 23 None -4 4 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1646 50 23 21 -4.1 CCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)C(C)C)CCCCN)Cc1c[nH]c2c1cccc2)CCCNC(=N)N)Cc1ccccc1)Cc1[nH]cnc1)CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CO)Cc1ccc(cc1)O)CO 10493100