Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL569693 mshr_human Human No 11.0 EC50 = 0.0 Funct
Agonistic activity against human MC1RAgonistic activity against human MC1R
789 22 8 7 1.6 C1C=NC=C1CC(C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)CCCC5=CC=CC=C5
CHEMBL569693 mshr_human Human No 11.0 EC50 = 0.0 Funct
Agonistic activity against human MC1RAgonistic activity against human MC1R
789 22 8 7 1.6 C1C=NC=C1CC(C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)CCCC5=CC=CC=C5
CHEMBL428615 mshr_human Human No 10.8 EC50 = 0.0 Funct
Evaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assayEvaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assay
1042 17 13 12 0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)F)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL428615 mshr_human Human No 10.8 EC50 = 0.0 Funct
Evaluated for agonist activity at cloned mammalian human MSH1 receptorEvaluated for agonist activity at cloned mammalian human MSH1 receptor
1042 17 13 12 0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)F)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL386081 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
1451 46 21 20 -4.6 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N)NC(=O)C(CO)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CO)NC(=O)C
CHEMBL3629347 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
1647 51 23 22 -3.5 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL3629347 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
1647 51 23 22 -3.5 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL2114259 mshr_human Human No 10.7 EC50 = 0.0 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1679 50 22 23 -4.3 CC(C)C(C(=O)N)NC(=O)C1CCCN1C(=O)C(CCCCN)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCCN=C(N)N)NC(=O)C(C(C)C4=CC=CC=C4)NC(=O)C(CC5=CNC=N5)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL216295 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1040 16 13 13 0.3 CC(C)CC(C(=O)NC1CC(=O)ONCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL386583 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
1025 21 12 13 -1.9 CCCCC(C(=O)N1C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C1=O)CCCCN)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)CC(=O)O)NC(=O)C
CHEMBL429236 mshr_mouse Mouse No 10.7 EC50 = 0.0 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
1310 40 16 16 -2.3 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C
CHEMBL428615 mshr_mouse Mouse No 10.6 EC50 = 0.0 Funct
Evaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assayEvaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assay
1042 17 13 12 0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)F)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL267794 mshr_mouse Mouse No 10.5 EC50 = 0.0 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
928 28 12 11 0.4 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C
CHEMBL2096742 mshr_human Human No 10.4 EC50 = 0.0 Funct
Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL266417 mshr_human Human No 10.4 EC50 = 0.0 Funct
Evaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assayEvaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL266417 mshr_human Human No 10.4 EC50 = 0.0 Funct
Evaluated for agonist activity at cloned mammalian human MSH1 receptorEvaluated for agonist activity at cloned mammalian human MSH1 receptor
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL410763 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
1265 38 18 17 -1.2 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C(CO)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CO)NC(=O)C
CHEMBL266417 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
Evaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assayEvaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3629347 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
1647 51 23 22 -3.5 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL2371851 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
1025 21 12 13 -1.9 CCCCC(C(=O)N1C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C1=O)CCCCN)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)CC(=O)O)NC(=O)C
CHEMBL3629347 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
1647 51 23 22 -3.5 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL2371851 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
1025 21 12 13 -1.9 CCCCC(C(=O)N1C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C1=O)CCCCN)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)CC(=O)O)NC(=O)C
CHEMBL377465 mshr_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL377465 mshr_human Human No 10.4 EC50 = 0.0 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL264536 mshr_mouse Mouse No 10.4 EC50 = 0.0 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
985 30 13 12 -0.2 CCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N)NC(=O)C
CHEMBL414965 mshr_mouse Mouse No 10.3 EC50 = 0.0 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1117 18 15 13 -0.9 CC(C(C(=O)N)NC(=O)C1CCCCNC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL266665 mshr_human Human No 10.3 EC50 = 0.1 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
965 27 10 9 2.9 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC5=CN=CN5)NC(=O)CCCC(=O)C6=CC=CC=C6
CHEMBL266665 mshr_human Human No 10.3 EC50 = 0.1 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
965 27 10 9 2.9 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC5=CN=CN5)NC(=O)CCCC(=O)C6=CC=CC=C6
CHEMBL440801 mshr_human Human No 10.3 EC50 = 0.1 Funct
Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor
1150 17 13 11 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)I)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL428801 mshr_human Human No 10.3 EC50 = 0.1 Funct
Evaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assayEvaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assay
1150 17 13 11 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)I)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL428801 mshr_human Human No 10.3 EC50 = 0.1 Funct
Evaluated for agonist activity at cloned mammalian human MSH1 receptorEvaluated for agonist activity at cloned mammalian human MSH1 receptor
1150 17 13 11 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)I)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3350330 mshr_human Human No 10.2 EC50 = 0.1 Funct
Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL212614 mshr_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
737 16 6 7 1.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL413912 mshr_human Human No 10.2 EC50 = 0.1 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
1647 49 22 22 -4.0 CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL212614 mshr_human Human No 10.2 EC50 = 0.1 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
737 16 6 7 1.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL413912 mshr_human Human No 10.2 EC50 = 0.1 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
1647 49 22 22 -4.0 CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)NC(CCCCN)C(=O)N5CCCC5C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL3358549 mshr_mouse Mouse No 10.1 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCN2C=C(CCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358549 mshr_mouse Mouse No 10.1 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCN2C=C(CCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358546 mshr_mouse Mouse No 10.1 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCCC2=CN(CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358546 mshr_mouse Mouse No 10.1 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCCC2=CN(CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2070241 mshr_human Human Yes 10.0 EC50 = 0.1 Funct
Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
1025 17 13 12 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)O)NC(=O)C
CHEMBL2115441 mshr_human Human No 10.0 EC50 = 0.1 Funct
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor
1095 17 14 12 -0.2 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C)C(=O)N)NC(=O)C
CHEMBL3358545 mshr_mouse Mouse No 10.0 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCC2=CN(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2372570 mshr_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
1024 17 12 11 -0.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=NC=NC2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3358545 mshr_mouse Mouse No 10.0 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCC2=CN(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2372570 mshr_human Human No 10.0 EC50 = 0.1 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
1024 17 12 11 -0.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=NC=NC2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL2112918 mshr_human Human No 10.0 EC50 = 0.1 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
815 24 10 9 0.5 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)OCC)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL405087 mshr_human Human No 10.0 EC50 = 0.1 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1096 18 14 14 -0.6 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL414965 mshr_human Human No 10.0 EC50 = 0.1 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1117 18 15 13 -0.9 CC(C(C(=O)N)NC(=O)C1CCCCNC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL428615 mshr_human Human No 10.0 EC50 = 0.1 Funct
Evaluated for agonist at cloned mammalian Melanocortin 1 receptor in frog (Rana pipiens) skin assayEvaluated for agonist at cloned mammalian Melanocortin 1 receptor in frog (Rana pipiens) skin assay
1042 17 13 12 0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)F)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3358544 mshr_mouse Mouse No 10.0 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCC2=CN(CCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358544 mshr_mouse Mouse No 10.0 EC50 = 0.1 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCC2=CN(CCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL269274 mshr_mouse Mouse No 9.8 EC50 = 0.2 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
4418 53 53 70 -7.4 CC1C(=O)NC(C(=O)NC2CSSSSCC3C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)NC(CSSSSCC(NC(=O)C(NC(=O)C5CSSSSCC(C(=O)NC(C(=O)NN(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N5)CC6=CC=CC=C6)C)CC(=O)N)CC7=CNC8=CC=CC=C87)CCCN=C(N)N)CC9=CC=CC=C9)CC4=CNC=N4)NC(=O)C(NC2=O)CC2=CC=C(C=C2)O)CC2=CC=C(C=C2)O)C(=O)NC(CCCN=C(N)N)C(=O)C(=O)N)C(=O)NC(CSSSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N3)CO)CCC(=O)O)CC2=CNC=N2)CC(C)C)CCCN=C(N)N)C(C)C)NNC(=O)C)C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)C)CC(=O)O)C(C)C)CCC(=O)N)CCC(=O)N)CC(C)C)C(C)O
CHEMBL428801 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Evaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assayEvaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assay
1150 17 13 11 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)I)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL13910 mshr_human Human No 9.7 EC50 = 0.2 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
650 14 3 6 4.7 CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)C(CC3=CN=CN3)NC(=O)C4=CC=CC=C4)C5=CC=CC=C5
CHEMBL263948 mshr_human Human Yes 9.7 EC50 = 0.2 Funct
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor
1665 51 23 23 -4.3 CC(C)C(C(=O)N)NC(=O)C1CCCN1C(=O)C(CCCCN)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC5=CN=CN5)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL3358552 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1034 17 12 12 0.1 CCCCC(C(=O)NC1CCN2C=C(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2369964 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1498 23 18 19 -1.6 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL3358552 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1034 17 12 12 0.1 CCCCC(C(=O)NC1CCN2C=C(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2115248 mshr_human Human No 9.7 EC50 = 0.2 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1679 50 22 23 -4.3 CC(C)C(C(=O)N)NC(=O)C1CCCN1C(=O)C(CCCCN)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCCN=C(N)N)NC(=O)C(C(C)C4=CC=CC=C4)NC(=O)C(CC5=CNC=N5)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL3350299 mshr_human Human No 9.7 EC50 = 0.2 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1679 50 22 23 -4.3 CC(C)C(C(=O)N)NC(=O)C1CCCN1C(=O)C(CCCCN)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCCN=C(N)N)NC(=O)C(C(C)C4=CC=CC=C4)NC(=O)C(CC5=CNC=N5)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CO)NC(=O)C
CHEMBL2369964 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1498 23 18 19 -1.6 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369484 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1529 24 22 22 -3.2 CC1C(=O)NC(C(=O)NC(NC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NNC6CC7=C(C=C(C=C7)O)NC6=O)C(=O)NNC(CC8=CC=C(C=C8)O)C(=O)C(=O)O)CC9=CC=CC=C9
CHEMBL2369959 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1487 23 19 19 -2.8 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369959 mshr_mouse Mouse No 9.7 EC50 = 0.2 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1487 23 19 19 -2.8 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL405087 mshr_mouse Mouse No 9.6 EC50 = 0.2 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1096 18 14 14 -0.6 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL3358537 mshr_mouse Mouse No 9.6 EC50 = 0.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 33 12 12 2.5 CCCCC(C(=O)NC(CCCCN=[N+]=[N-])C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC#C)C(=O)N)NC(=O)C
CHEMBL3358537 mshr_mouse Mouse No 9.6 EC50 = 0.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 33 12 12 2.5 CCCCC(C(=O)NC(CCCCN=[N+]=[N-])C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC#C)C(=O)N)NC(=O)C
CHEMBL3358541 mshr_mouse Mouse No 9.6 EC50 = 0.3 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1038 33 12 12 3.0 CCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL3358541 mshr_mouse Mouse No 9.6 EC50 = 0.3 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1038 33 12 12 3.0 CCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL379508 mshr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL3037885 mshr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1015 18 13 11 -0.9 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C
CHEMBL393075 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effect on human MC1R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC1R expressed in HEK293 cells assessed as intracellular cAMP accumulation
1032 16 13 11 1.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N
CHEMBL2369973 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1613 23 19 19 -2.1 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=C(C=C4)I)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL379508 mshr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL3037885 mshr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1015 18 13 11 -0.9 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C
CHEMBL1688107 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1507 24 20 19 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCNC(=N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)N)CC8=CC=CC=C8
CHEMBL393075 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effect on human MC1R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC1R expressed in HEK293 cells assessed as intracellular cAMP accumulation
1032 16 13 11 1.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N
CHEMBL2364555 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generationEffective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3350396 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor
1095 17 14 12 -0.2 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C)C(=O)N)NC(=O)C
CHEMBL2369973 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1613 23 19 19 -2.1 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=C(C=C4)I)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2370906 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.
1056 33 14 13 -2.4 CCCCC(C(=O)NC(CC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(C(C)C3=CNC4=CC=CC=C43)C(=O)NC(CCCCN)C(=O)N)NC(=O)C
CHEMBL407098 mshr_human Human No 9.5 EC50 = 0.3 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1110 18 14 14 -0.2 CC(C(C(=O)N)NC(=O)C1CSSCCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=NC=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL3358551 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1034 17 12 12 0.1 CCCCC(C(=O)NC1CCC2=CN(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358551 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1034 17 12 12 0.1 CCCCC(C(=O)NC1CCC2=CN(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL191303 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
770 24 9 7 3.0 CCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3350329 mshr_human Human No 9.5 EC50 = 0.3 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL191303 mshr_mouse Mouse No 9.5 EC50 = 0.3 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
770 24 9 7 3.0 CCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL1688107 mshr_mouse Mouse No 9.5 EC50 = 0.4 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1507 24 20 19 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCNC(=N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)N)CC8=CC=CC=C8
CHEMBL1688107 mshr_mouse Mouse No 9.5 EC50 = 0.4 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1507 24 20 19 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCNC(=N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)N)CC8=CC=CC=C8
CHEMBL275067 mshr_human Human No 9.5 EC50 = 0.4 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
588 13 3 6 3.0 CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)C(CC3=CN=CN3)NC(=O)C)C4=CC=CC=C4
CHEMBL3358539 mshr_mouse Mouse No 9.4 EC50 = 0.4 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.5 CCCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL3358539 mshr_mouse Mouse No 9.4 EC50 = 0.4 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.5 CCCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL215833 mshr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
746 17 6 8 0.8 CC(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCN(C(=O)C2CCCN=C(N)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL215833 mshr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
746 17 6 8 0.8 CC(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCN(C(=O)C2CCCN=C(N)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL406842 mshr_mouse Mouse No 9.4 EC50 = 0.4 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1131 18 14 14 0.1 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=C(C=C4)Cl)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL24892 mshr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
953 15 12 10 0.2 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL195439 mshr_mouse Mouse No 9.4 EC50 = 0.4 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
784 25 9 7 3.5 CCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL24892 mshr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
953 15 12 10 0.2 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL2370906 mshr_human Human No 9.4 EC50 = 0.4 Funct
Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generationEffective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation
1056 33 14 13 -2.4 CCCCC(C(=O)NC(CC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(C(C)C3=CNC4=CC=CC=C43)C(=O)NC(CCCCN)C(=O)N)NC(=O)C
CHEMBL345234 mshr_human Human No 9.4 EC50 = 0.4 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
801 23 10 9 0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)OC)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL195439 mshr_mouse Mouse No 9.4 EC50 = 0.4 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
784 25 9 7 3.5 CCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2115249 mshr_human Human No 9.4 EC50 = 0.4 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL2364555 mshr_human Human No 9.4 EC50 = 0.4 Funct
Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3358533 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 33 12 12 2.5 CCCCC(C(=O)NC(CC#C)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL2372859 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1042 33 14 13 -2.7 CCCCC(C(=O)NC(CC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCN)C(=O)N)NC(=O)C
CHEMBL3358533 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 33 12 12 2.5 CCCCC(C(=O)NC(CC#C)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL2372859 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1042 33 14 13 -2.7 CCCCC(C(=O)NC(CC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCN)C(=O)N)NC(=O)C
CHEMBL405335 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
1067 30 13 12 -0.4 CC(C)C(C(=O)N)NC(=O)C1CCCN1C(=O)C(CCCCN)NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC5=CN=CN5)NC(=O)C
CHEMBL2323795 mshr_mouse Mouse Yes 9.3 EC50 = 0.5 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1762 24 22 33 6.2 CC1C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=N1)O)CC(=N)O)O)CC3=CNC4=CC=CC=C43)O)CC5=CC=C(C=C5)I)O)CC6=CN=CN6)O)N=C(C(CC7=CC=C(C=C7)O)N)O)C(=NC(CC8=CC=C(C=C8)O)C(=N)O)O)O)CC9=CC=CC=C9)O
CHEMBL432565 mshr_human Human No 9.3 EC50 = 0.5 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
776 21 9 7 1.9 C1=CC=C(C=C1)CCC(=O)NC(CC2=CN=CN2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL3358540 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.7 CCCCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL3358550 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CN2C=C(CCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2369963 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1498 23 18 19 -1.6 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL3358540 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.7 CCCCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL3358550 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CN2C=C(CCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL2369963 mshr_mouse Mouse No 9.3 EC50 = 0.5 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1498 23 18 19 -1.6 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL370261 mshr_mouse Mouse No 9.2 EC50 = 0.6 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
854 30 9 7 6.2 CCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL370261 mshr_mouse Mouse No 9.2 EC50 = 0.6 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
854 30 9 7 6.2 CCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3422426 mshr_mouse Mouse Yes 9.2 EC50 = 0.6 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL2096742 mshr_mouse Mouse No 9.2 EC50 = 0.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3422426 mshr_mouse Mouse Yes 9.2 EC50 = 0.6 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL2096742 mshr_mouse Mouse No 9.2 EC50 = 0.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3422426 mshr_mouse Mouse Yes 9.2 EC50 = 0.7 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3422426 mshr_mouse Mouse Yes 9.2 EC50 = 0.7 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3358548 mshr_mouse Mouse No 9.2 EC50 = 0.7 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCN2C=C(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358548 mshr_mouse Mouse No 9.2 EC50 = 0.7 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCN2C=C(CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358534 mshr_mouse Mouse No 9.1 EC50 = 0.7 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.3 CCCCC(C(=O)NC(CCCC)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL191304 mshr_mouse Mouse No 9.1 EC50 = 0.7 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
896 33 9 7 7.9 CCCCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3358534 mshr_mouse Mouse No 9.1 EC50 = 0.7 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.3 CCCCC(C(=O)NC(CCCC)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL191304 mshr_mouse Mouse No 9.1 EC50 = 0.7 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
896 33 9 7 7.9 CCCCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3358542 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1083 33 14 12 -0.9 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCNC(=O)C)C(=O)N)NC(=O)C
CHEMBL3358542 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1083 33 14 12 -0.9 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCNC(=O)C)C(=O)N)NC(=O)C
CHEMBL3358535 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.5 CCCCCC(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCN=[N+]=[N-])C(=O)N)NC(=O)C(CCCC)NC(=O)C
CHEMBL3358535 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.5 CCCCCC(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCN=[N+]=[N-])C(=O)N)NC(=O)C(CCCC)NC(=O)C
CHEMBL3358538 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.3 CCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL364726 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
896 35 9 7 9.1 CCCCCCCCCCCCCCCCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3358538 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.3 CCCCC(C(=O)N)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C(CCCN=[N+]=[N-])NC(=O)C(CCCC)NC(=O)C
CHEMBL364726 mshr_mouse Mouse No 9.1 EC50 = 0.8 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
896 35 9 7 9.1 CCCCCCCCCCCCCCCCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3358547 mshr_mouse Mouse No 9.1 EC50 = 0.9 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCCN2C=C(CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL3358547 mshr_mouse Mouse No 9.1 EC50 = 0.9 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1048 17 12 12 0.5 CCCCC(C(=O)NC1CCCCN2C=C(CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)N=N2)NC(=O)C
CHEMBL190366 mshr_mouse Mouse No 9.0 EC50 = 0.9 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
840 29 9 7 5.7 CCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL190366 mshr_mouse Mouse No 9.0 EC50 = 0.9 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
840 29 9 7 5.7 CCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3735607 mshr_mouse Mouse No 9.0 EC50 = 1.0 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3735607 mshr_mouse Mouse No 9.0 EC50 = 1.0 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL265236 mshr_mouse Mouse No 9.0 EC50 = 1.0 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
882 32 9 7 7.3 CCCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL265236 mshr_mouse Mouse No 9.0 EC50 = 1.0 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
882 32 9 7 7.3 CCCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL412358 mshr_human Human No 9.0 EC50 = 1 Funct
Agonist potency for human Melanocortin 1 receptorAgonist potency for human Melanocortin 1 receptor
771 22 10 8 0.9 CCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCC(=O)N=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL319752 mshr_human Human No 9.0 EC50 = 1 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
967 15 11 12 -1.5 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C2CSCCN2C(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)C(=O)N)NC(=O)C
CHEMBL3350330 mshr_human Human No 9.0 EC50 = 1 Funct
Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generationEffective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL2112917 mshr_human Human No 9.0 EC50 = 1 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
801 22 9 8 1.3 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC(=C(C=C3)Cl)Cl)C(=O)NCC(=O)N
CHEMBL427814 mshr_human Human No 9.0 EC50 = 1 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1145 18 15 13 -0.2 CC1=NC=C(N1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CCCCNC(=O)CCC(C(=O)N2)NC(=O)C(CC3=CC=CC=C3)N)C(=O)NC(C(C)O)C(=O)N)CC4=CNC5=CC=CC=C54)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL2323796 mshr_mouse Mouse Yes 9.0 EC50 = 1.1 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1712 25 22 33 7.2 CC1C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=N1)O)CC(=N)O)O)CC3=CNC4=CC=CC=C43)O)CC5=CC=C(C=C5)C6=CC=CC=C6)O)CC7=CN=CN7)O)N=C(C(CC8=CC=C(C=C8)O)N)O)C(=NC(CC9=CC=C(C=C9)O)C(=N)O)O)O)CC1=CC=CC=C1)O
CHEMBL3358536 mshr_mouse Mouse No 8.9 EC50 = 1.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.7 CCCCCCC(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CN=[N+]=[N-])C(=O)N)NC(=O)C(CCCC)NC(=O)C
CHEMBL3358536 mshr_mouse Mouse No 8.9 EC50 = 1.2 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1052 34 12 12 3.7 CCCCCCC(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CN=[N+]=[N-])C(=O)N)NC(=O)C(CCCC)NC(=O)C
CHEMBL3735607 mshr_mouse Mouse No 8.9 EC50 = 1.4 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL503229 mshr_human Human Yes 8.8 EC50 = 1.5 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 minsAgonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins
1594 50 23 19 1.1 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C
CHEMBL2096742 mshr_human Human No 8.8 EC50 = 1.5 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL503229 mshr_human Human Yes 8.8 EC50 = 1.5 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1594 50 23 19 1.1 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C
CHEMBL2096742 mshr_human Human No 8.8 EC50 = 1.5 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL503229 mshr_human Human Yes 8.8 EC50 = 1.5 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1594 50 23 19 1.1 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C
CHEMBL414778 mshr_human Human No 8.8 EC50 = 1.5 Funct
Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)
1579 48 20 21 -0.9 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC=CC=C4)C(=O)NC(CC(=O)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)ON)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)N
CHEMBL443071 mshr_human Human No 8.8 EC50 = 1.5 Funct
Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)
1610 49 21 21 -1.7 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)ON)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C
CHEMBL446941 mshr_human Human No 8.8 EC50 = 1.5 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
546 12 3 6 2.8 CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)C(CC3=CN=CN3)N)C4=CC=CC=C4
CHEMBL410404 mshr_mouse Mouse No 8.8 EC50 = 1.5 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1096 18 14 14 -0.6 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL598214 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 5 1 5 4.3 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC(=CC5=NN4)F)C6=CC=CC=C6
CHEMBL590281 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
556 8 1 6 4.3 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL605115 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
520 5 1 4 4.2 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC=CC5=NN4)C6=CC=CC=C6
CHEMBL599867 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
520 5 1 4 4.2 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC=CC5=NN4)C6=CC=CC=C6
CHEMBL598214 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 5 1 5 4.3 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC(=CC5=NN4)F)C6=CC=CC=C6
CHEMBL590281 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
556 8 1 6 4.3 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL605115 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
520 5 1 4 4.2 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC=CC5=NN4)C6=CC=CC=C6
CHEMBL599867 mshr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
520 5 1 4 4.2 C1CCN(C2=CC=CC=C2C1)C(=O)CN3C=CN(C(=O)C(C3=O)CC4=C5C=CC=CC5=NN4)C6=CC=CC=C6
CHEMBL569693 mshr_mouse Mouse No 8.8 EC50 = 1.6 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
789 22 8 7 1.6 C1C=NC=C1CC(C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)CCCC5=CC=CC=C5
CHEMBL569693 mshr_mouse Mouse No 8.8 EC50 = 1.6 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
789 22 8 7 1.6 C1C=NC=C1CC(C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)CCCC5=CC=CC=C5
CHEMBL384774 mshr_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
755 16 6 8 1.8 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL379054 mshr_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
763 16 6 7 3.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL384774 mshr_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
755 16 6 8 1.8 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL379054 mshr_human Human No 8.8 EC50 = 1.7 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
763 16 6 7 3.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCN(C(=O)C3CCCN=C(N)N)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL2323789 mshr_mouse Mouse Yes 8.7 EC50 = 1.9 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1646 24 21 32 7.4 CC1C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=N1)O)CC(=N)O)O)CC3=CNC4=CC=CC=C43)O)CC5=CC=CC=C5)O)CC6=CC=CC=C6)O)N=C(C(CC7=CC=C(C=C7)O)N)O)C(=NC(CC8=CC=C(C=C8)O)C(=N)O)O)O)CC9=CC=CC=C9)O
CHEMBL3352878 mshr_mouse Mouse No 8.7 EC50 = 2.0 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1038 33 12 12 3.0 CCCCC(C(=O)NC(CCCC)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL3352878 mshr_mouse Mouse No 8.7 EC50 = 2.0 Funct
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
1038 33 12 12 3.0 CCCCC(C(=O)NC(CCCC)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCN=[N+]=[N-])C(=O)N)NC(=O)C
CHEMBL506762 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
630 11 3 6 4.4 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCNCC3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity against human melanocortin receptor hMC1R at 50% maximum cAMP accumulationAgonist activity against human melanocortin receptor hMC1R at 50% maximum cAMP accumulation
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL506762 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
630 11 3 6 4.4 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCNCC3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL78565 mshr_human Human No 8.0 EC50 = 10 Funct
Agonist potency for human Melanocortin 1 receptorAgonist potency for human Melanocortin 1 receptor
757 23 10 8 0.9 CCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL2371219 mshr_human Human No 8.0 EC50 = 10 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
840 22 10 8 1.4 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC(=C(C=C2)Cl)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL349298 mshr_human Human No 8.0 EC50 = 10 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL29582 mshr_human Human No 8.0 EC50 = 10 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL410404 mshr_human Human No 8.0 EC50 = 10 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1096 18 14 14 -0.6 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL508068 mshr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulation
894 11 10 11 1.2 C1C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2=C(S1)C=CC(=C2)[N+](=O)[O-])CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL488355 mshr_mouse Mouse No 7.0 EC50 = 100 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
742 19 9 7 1.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C(C)(C)C)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL508068 mshr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulation
894 11 10 11 1.2 C1C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2=C(S1)C=CC(=C2)[N+](=O)[O-])CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL488355 mshr_mouse Mouse No 7.0 EC50 = 100 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
742 19 9 7 1.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C(C)(C)C)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL507214 mshr_human Human Yes 7.0 EC50 = 100 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1062 16 14 15 0.5 CC(C1C(=O)NC(C(SSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)N)(C)C)C(=O)NC(C(C)O)C(=O)N)O
CHEMBL415200 mshr_human Human No 7.0 EC50 = 100 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1054 17 12 14 -0.2 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)N(CC(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL203602 mshr_human Human Yes 6.0 EC50 = 1000 Funct
Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation
859 15 11 9 -0.3 CCCCC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CCC(=O)N1)C(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CCC(=O)N
CHEMBL3421679 mshr_human Human No 6.0 EC50 = 1000 Funct
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
708 15 7 6 1.6 CC(=O)NC1CC2=CC=CC=C2CN(C1=O)C(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL602654 mshr_mouse Mouse No 6.0 EC50 = 1000 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
850 12 8 8 0.4 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)CN(C(=O)C(NC(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL2369962 mshr_mouse Mouse No 6.0 EC50 = 1000 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1398 21 17 19 -4.2 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)CC(=O)N)CCCN=C(N)N)CC3=CC=CC=C3)CC4=CNC=N4)NC(=O)C(CC5=CC=C(C=C5)O)N)C(CC6=CC=C(C=C6)O)C(=O)N)(C)C(=O)O)CC7=CC=CC=C7
CHEMBL203602 mshr_human Human Yes 6.0 EC50 = 1000 Funct
Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation
859 15 11 9 -0.3 CCCCC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CCC(=O)N1)C(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CCC(=O)N
CHEMBL3421679 mshr_human Human No 6.0 EC50 = 1000 Funct
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
708 15 7 6 1.6 CC(=O)NC1CC2=CC=CC=C2CN(C1=O)C(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL602654 mshr_mouse Mouse No 6.0 EC50 = 1000 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
850 12 8 8 0.4 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)CN(C(=O)C(NC(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL2369962 mshr_mouse Mouse No 6.0 EC50 = 1000 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1398 21 17 19 -4.2 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)CC(=O)N)CCCN=C(N)N)CC3=CC=CC=C3)CC4=CNC=N4)NC(=O)C(CC5=CC=C(C=C5)O)N)C(CC6=CC=C(C=C6)O)C(=O)N)(C)C(=O)O)CC7=CC=CC=C7
CHEMBL406891 mshr_human Human No 6.0 EC50 = 1000 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1110 18 14 14 -0.2 CC(C(C(=O)N)NC(=O)C1CCSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL411009 mshr_human Human No 6.0 EC50 = 1000 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1114 18 14 15 -0.5 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=C(C=C4)F)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL432895 mshr_mouse Mouse Yes 5.0 EC50 = 10000 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
549 14 7 5 0.2 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N
CHEMBL432895 mshr_mouse Mouse Yes 5.0 EC50 = 10000 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
549 14 7 5 0.2 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N
CHEMBL405791 mshr_human Human No 5.0 EC50 = 10000 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1146 18 14 14 0.7 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC5=CC=CC=C54)CC6=NC=CN6)NC(=O)C(CC7=CC=CC=C7)N)O
CHEMBL411378 mshr_human Human No 5.0 EC50 = 10000 Funct
Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.
1110 18 14 14 -0.2 CC1=NC=C(N1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)N2)NC(=O)C(CC3=CC=CC=C3)N)C(=O)NC(C(C)O)C(=O)N)CC4=CNC5=CC=CC=C54)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL136066 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
658 17 8 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCC(=O)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL137774 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
464 10 5 4 1.2 CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C
CHEMBL422994 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
587 14 7 6 0.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NCC(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL138959 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
601 14 7 6 0.7 CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CN=CN4)NC(=O)C
CHEMBL335807 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
521 14 6 5 1.2 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCCN)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N
CHEMBL336027 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
521 13 6 5 0.2 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCC(=O)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N
CHEMBL335790 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
450 10 5 4 1.0 CC(=O)NC(CC1=CC=CC=C1)C(=O)NCC(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N
CHEMBL344489 mshr_mouse Mouse No 4.0 EC50 = 100000 Funct
Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)Agonistic activity against mouse Melanocortin 1 receptor (mMC1R)
658 18 8 7 0.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCCN)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL1093304 mshr_human Human No 6.0 EC50 = 1020 Funct
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
600 5 1 5 5.8 CC1=C(C=C2C(=C1)C(CC23CCN(CC3)C(=O)C4CN(CC4C5=C(C=C(C=C5)F)F)C(C)(C)C)C(C)(C)NC(=O)C)Cl
CHEMBL1093304 mshr_human Human No 6.0 EC50 = 1020 Funct
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
600 5 1 5 5.8 CC1=C(C=C2C(=C1)C(CC23CCN(CC3)C(=O)C4CN(CC4C5=C(C=C(C=C5)F)F)C(C)(C)C)C(C)(C)NC(=O)C)Cl
CHEMBL184968 mshr_human Human No 6.0 EC50 = 1028 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
788 21 8 8 3.1 CCC(=O)OC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL184968 mshr_human Human No 6.0 EC50 = 1028 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
788 21 8 8 3.1 CCC(=O)OC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL451423 mshr_mouse Mouse No 6.0 EC50 = 1030 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
731 18 9 9 -0.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)[N+](=O)[O-])C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL451423 mshr_mouse Mouse No 6.0 EC50 = 1030 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
731 18 9 9 -0.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)[N+](=O)[O-])C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2369972 mshr_mouse Mouse No 5.0 EC50 = 10300 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1437 21 18 19 -4.0 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369972 mshr_mouse Mouse No 5.0 EC50 = 10300 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1437 21 18 19 -4.0 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL215895 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
735 13 5 7 3.4 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)N3CCN(C(C3=O)CCCN=C(N)N)C(=O)C(CC4=CC=C(C=C4)F)NC(=O)C5CC6=CC=CC=C6CN5
CHEMBL506272 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
630 11 3 6 3.8 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCC(=O)N3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL377778 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
614 12 5 6 1.7 C1CNCCC1C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL215895 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
735 13 5 7 3.4 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)N3CCN(C(C3=O)CCCN=C(N)N)C(=O)C(CC4=CC=C(C=C4)F)NC(=O)C5CC6=CC=CC=C6CN5
CHEMBL506272 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
630 11 3 6 3.8 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCC(=O)N3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL377778 mshr_human Human No 7.0 EC50 = 104 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
614 12 5 6 1.7 C1CNCCC1C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL421028 mshr_mouse Mouse No 5.0 EC50 = 10600 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
762 19 9 7 1.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL210009 mshr_human Human No 6.0 EC50 = 1070 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
585 12 4 5 3.6 C1CCNC(C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL210009 mshr_human Human No 6.0 EC50 = 1070 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
585 12 4 5 3.6 C1CCNC(C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL466380 mshr_human Human No 6.0 EC50 = 1076 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
561 10 2 5 4.3 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL466380 mshr_human Human No 6.0 EC50 = 1076 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
561 10 2 5 4.3 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL568577 mshr_mouse Mouse No 6.0 EC50 = 1080 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
622 16 7 6 1.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=C(C=C3)Cl
CHEMBL568577 mshr_mouse Mouse No 6.0 EC50 = 1080 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
622 16 7 6 1.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=C(C=C3)Cl
CHEMBL405282 mshr_mouse Mouse Yes 6.0 EC50 = 1090 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1571 49 23 21 -1.6 CC(C)C(C(=O)NC(CCSC)C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)O)NC(=O)C(CC6=CC=C(C=C6)O)N
CHEMBL405282 mshr_mouse Mouse Yes 6.0 EC50 = 1090 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1571 49 23 21 -1.6 CC(C)C(C(=O)NC(CCSC)C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)O)NC(=O)C(CC6=CC=C(C=C6)O)N
CHEMBL2369965 mshr_mouse Mouse No 7.9 EC50 = 11.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1524 24 18 19 -1.3 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=C(C=C2)C3=CC=CC=C3)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369965 mshr_mouse Mouse No 7.9 EC50 = 11.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1524 24 18 19 -1.3 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=C(C=C2)C3=CC=CC=C3)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2111251 mshr_human Human No 7.0 EC50 = 110 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
771 22 10 8 -0.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL1090484 mshr_human Human No 6.0 EC50 = 1100 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
471 6 1 5 4.7 CCCCN1CC(C(C1)C(=O)N2CC(C(C(C2)C)(C3=CC=CC=C3)O)C)C4=C(C=C(C=C4)F)F
CHEMBL1090484 mshr_human Human No 6.0 EC50 = 1100 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
471 6 1 5 4.7 CCCCN1CC(C(C1)C(=O)N2CC(C(C(C2)C)(C3=CC=CC=C3)O)C)C4=C(C=C(C=C4)F)F
CHEMBL3799408 mshr_mouse Mouse No 7.0 EC50 = 112 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1054 36 11 13 0.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.0 EC50 = 112 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3799408 mshr_mouse Mouse No 7.0 EC50 = 112 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1054 36 11 13 0.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.0 EC50 = 112 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL1204061 mshr_human Human No 6.0 EC50 = 1120 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
489 4 1 6 4.6 CC1CN(CC(C1(C2=CC=C(C=C2)F)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C
CHEMBL565740 mshr_mouse Mouse No 6.0 EC50 = 1120 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 17 8 7 0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CC(=CC=C3)O
CHEMBL1204061 mshr_human Human No 6.0 EC50 = 1120 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
489 4 1 6 4.6 CC1CN(CC(C1(C2=CC=C(C=C2)F)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C
CHEMBL565740 mshr_mouse Mouse No 6.0 EC50 = 1120 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 17 8 7 0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CC(=CC=C3)O
CHEMBL361253 mshr_human Human No 7.0 EC50 = 113 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
834 22 8 6 4.4 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL361253 mshr_human Human No 7.0 EC50 = 113 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
834 22 8 6 4.4 C1=CC=C(C=C1)CCCC(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL275303 mshr_mouse Mouse No 5.0 EC50 = 11300 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
708 15 7 6 1.6 CC(=O)N1CC2=CC=CC=C2CC1C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL363061 mshr_human Human No 6.9 EC50 = 114 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
866 22 8 8 3.8 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CCC(=O)C5=CC=C(C=C5)F
CHEMBL363061 mshr_human Human No 6.9 EC50 = 114 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
866 22 8 8 3.8 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CCC(=O)C5=CC=C(C=C5)F
CHEMBL3600835 mshr_human Human No 6.9 EC50 = 115 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1088 17 12 11 1.5 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600835 mshr_human Human No 6.9 EC50 = 115 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1088 17 12 11 1.5 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL317969 mshr_mouse Mouse No 5.9 EC50 = 1150 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
697 18 8 7 0.5 CC(=O)NC(CC1=CN=CC=C1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL329847 mshr_mouse Mouse No 4.9 EC50 = 11500 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
696 18 8 6 1.5 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3600842 mshr_human Human No 5.9 EC50 = 1160 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL566150 mshr_mouse Mouse No 5.9 EC50 = 1160 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 16 7 7 0.7 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=CC=C3F
CHEMBL567039 mshr_mouse Mouse No 5.9 EC50 = 1160 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 17 8 7 0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CC=C(C=C3)O
CHEMBL3600842 mshr_human Human No 5.9 EC50 = 1160 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL566150 mshr_mouse Mouse No 5.9 EC50 = 1160 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 16 7 7 0.7 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=CC=C3F
CHEMBL567039 mshr_mouse Mouse No 5.9 EC50 = 1160 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 17 8 7 0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CC=C(C=C3)O
CHEMBL3577980 mshr_mouse Mouse No 4.9 EC50 = 11600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1506 19 18 18 2.3 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CC5=CC=CC=C5)CCCNC(=N)N)C(C)O)CC6=CC=C(C=C6)O)CC7=CC=C(C=C7)O)C(C)O)CC8=CC=CC=C8
CHEMBL3577980 mshr_mouse Mouse No 4.9 EC50 = 11600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1506 19 18 18 2.3 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CC5=CC=CC=C5)CCCNC(=N)N)C(C)O)CC6=CC=C(C=C6)O)CC7=CC=C(C=C7)O)C(C)O)CC8=CC=CC=C8
CHEMBL3600922 mshr_human Human No 6.9 EC50 = 117 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600922 mshr_human Human No 6.9 EC50 = 117 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL1089830 mshr_human Human No 5.9 EC50 = 1170 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
472 4 1 6 3.4 CC1CN(CC(C1(C2=CC=CC=N2)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C
CHEMBL589517 mshr_mouse Mouse No 5.9 EC50 = 1170 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
864 12 8 8 0.7 C1CCC(=O)NC(C(=O)N(CC(=O)NC(C(=O)NC(C(=O)N(CCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL1089830 mshr_human Human No 5.9 EC50 = 1170 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
472 4 1 6 3.4 CC1CN(CC(C1(C2=CC=CC=N2)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C
CHEMBL589517 mshr_mouse Mouse No 5.9 EC50 = 1170 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
864 12 8 8 0.7 C1CCC(=O)NC(C(=O)N(CC(=O)NC(C(=O)NC(C(=O)N(CCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL3577977 mshr_mouse Mouse No 4.9 EC50 = 11700 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1832 39 27 25 -2.5 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCNC(=N)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C(C)O)NC(=O)C(C(C)O)NC(=O)C)C(=O)NC(CC5=CC=C(C=C5)O)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)N)CC6=CC=CC=C6
CHEMBL3577977 mshr_mouse Mouse No 4.9 EC50 = 11700 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1832 39 27 25 -2.5 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCNC(=N)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C(C)O)NC(=O)C(C(C)O)NC(=O)C)C(=O)NC(CC5=CC=C(C=C5)O)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)N)CC6=CC=CC=C6
CHEMBL3600841 mshr_human Human No 5.9 EC50 = 1171 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600841 mshr_human Human No 5.9 EC50 = 1171 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL591195 mshr_human Human No 5.9 EC50 = 1174.9 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
588 10 1 7 3.6 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)CC5=CC=CS5
CHEMBL591195 mshr_human Human No 5.9 EC50 = 1174.9 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
588 10 1 7 3.6 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)CC5=CC=CS5
CHEMBL568409 mshr_mouse Mouse No 5.9 EC50 = 1175 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
617 15 9 7 0.3 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C3=CC4=C(N3)C=CC(=C4)O
CHEMBL568409 mshr_mouse Mouse No 5.9 EC50 = 1175 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
617 15 9 7 0.3 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C3=CC4=C(N3)C=CC(=C4)O
CHEMBL1688105 mshr_mouse Mouse Yes 5.9 EC50 = 1180 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CNC=N3)C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CC=CC=C6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL1688105 mshr_mouse Mouse Yes 5.9 EC50 = 1180 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CNC=N3)C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CC=CC=C6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL602650 mshr_mouse Mouse No 4.9 EC50 = 11800 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 9 8 -0.1 CC(=O)NCC(=O)N(CC1=CC=CC=C1)CC(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL602650 mshr_mouse Mouse No 4.9 EC50 = 11800 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 9 8 -0.1 CC(=O)NCC(=O)N(CC1=CC=CC=C1)CC(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL1682208 mshr_human Human No 7.9 EC50 = 12 Funct
Agonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation
672 10 2 9 3.1 COCC(=O)NC1CC2=CC(=C3C(=C2)COCO3)CC4=CC=C(C=C4)OC5=CC=CC(=C5)CN(C1=O)CCCN6CCN(CC6)CCCN
CHEMBL410148 mshr_human Human No 7.9 EC50 = 12 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1031 15 11 12 2.9 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CC=C(C=C2)C(F)(F)F)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL3287323 mshr_mouse Mouse No 7.9 EC50 = 12 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
899 18 8 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)N
CHEMBL1682208 mshr_human Human No 7.9 EC50 = 12 Funct
Agonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation
672 10 2 9 3.1 COCC(=O)NC1CC2=CC(=C3C(=C2)COCO3)CC4=CC=C(C=C4)OC5=CC=CC(=C5)CN(C1=O)CCCN6CCN(CC6)CCCN
CHEMBL410148 mshr_human Human No 7.9 EC50 = 12 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1031 15 11 12 2.9 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CC=C(C=C2)C(F)(F)F)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL3287323 mshr_mouse Mouse No 7.9 EC50 = 12 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
899 18 8 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)N
CHEMBL590794 mshr_human Human No 7.9 EC50 = 12.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
557 8 1 7 3.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CN=CC=C5
CHEMBL590794 mshr_human Human No 7.9 EC50 = 12.6 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
557 8 1 7 3.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CN=CC=C5
CHEMBL3799955 mshr_mouse Mouse No 7.9 EC50 = 12.6 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1949 74 23 25 -0.8 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NC(CC5=CN=CN5)C(=O)NC(CC6=CC=CC=C6)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC7=CNC8=CC=CC=C87)C(=O)N
CHEMBL3799955 mshr_mouse Mouse No 7.9 EC50 = 12.6 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1949 74 23 25 -0.8 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NC(CC5=CN=CN5)C(=O)NC(CC6=CC=CC=C6)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC7=CNC8=CC=CC=C87)C(=O)N
CHEMBL526334 mshr_human Human Yes 6.9 EC50 = 120 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1535 44 19 18 2.2 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCCC3C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)C
CHEMBL406985 mshr_mouse Mouse No 6.9 EC50 = 120 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
850 12 9 8 0.7 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL3350327 mshr_mouse Mouse No 6.9 EC50 = 120 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
2327 55 32 33 -6.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCNC(=N)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C)NC(=O)C5CCCN5C(=O)C(CC(=O)O)N)C(=O)NC(CC6=CC=C(C=C6)O)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)O)CC7=CC=CC=C7
CHEMBL602853 mshr_mouse Mouse No 6.9 EC50 = 120 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
864 12 8 8 0.7 C1CCC(=O)N(CC(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(CCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL526334 mshr_human Human Yes 6.9 EC50 = 120 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1535 44 19 18 2.2 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CCCC3C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)C
CHEMBL406985 mshr_mouse Mouse No 6.9 EC50 = 120 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
850 12 9 8 0.7 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL602853 mshr_mouse Mouse No 6.9 EC50 = 120 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
864 12 8 8 0.7 C1CCC(=O)N(CC(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(CCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL1209318 mshr_human Human No 5.9 EC50 = 1200 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
625 9 0 8 4.9 CC(C)N(CC(C1CCCCC1)N2CCN(CC2)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C)C(=O)C5=NN=CC=C5
CHEMBL569695 mshr_mouse Mouse No 5.9 EC50 = 1200 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
588 16 7 6 0.6 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=CC=C3
CHEMBL1209318 mshr_human Human No 5.9 EC50 = 1200 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
625 9 0 8 4.9 CC(C)N(CC(C1CCCCC1)N2CCN(CC2)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C(C)(C)C)C(=O)C5=NN=CC=C5
CHEMBL569695 mshr_mouse Mouse No 5.9 EC50 = 1200 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
588 16 7 6 0.6 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC=CC=C3
CHEMBL3577992 mshr_mouse Mouse No 4.9 EC50 = 12100 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
999 10 9 10 1.4 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC4=CC5=CC=CC=C5C=C4C(=O)NC(C(=O)N1)CC(=O)N)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3577992 mshr_mouse Mouse No 4.9 EC50 = 12100 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
999 10 9 10 1.4 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC4=CC5=CC=CC=C5C=C4C(=O)NC(C(=O)N1)CC(=O)N)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL263047 mshr_human Human No 5.9 EC50 = 1214 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
798 19 8 9 3.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CC(F)(F)F
CHEMBL263047 mshr_human Human No 5.9 EC50 = 1214 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
798 19 8 9 3.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CC(F)(F)F
CHEMBL213747 mshr_human Human No 5.9 EC50 = 1220 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL27848 mshr_human Human No 5.9 EC50 = 1220 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
835 21 9 7 3.1 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2C)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL213747 mshr_human Human No 5.9 EC50 = 1220 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
653 15 5 6 2.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL568836 mshr_mouse Mouse No 5.9 EC50 = 1230 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
636 18 7 8 -0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC(=O)C3=CC=C(C=C3)F
CHEMBL568836 mshr_mouse Mouse No 5.9 EC50 = 1230 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
636 18 7 8 -0.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC(=O)C3=CC=C(C=C3)F
CHEMBL569076 mshr_mouse Mouse No 5.9 EC50 = 1250 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
624 16 7 8 0.8 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=C(C=C(C=C3)F)F
CHEMBL569076 mshr_mouse Mouse No 5.9 EC50 = 1250 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
624 16 7 8 0.8 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=C(C=C(C=C3)F)F
CHEMBL2323792 mshr_mouse Mouse Yes 4.9 EC50 = 12500 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1560 22 22 33 4.0 CC1C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=NC(C(=NC(C(=NC(CSSCC(C(=NC(C(=N1)O)CC3=CN=CN3)O)N=C(C(CC4=CC=C(C=C4)O)N)O)C(=NC(CC5=CC=C(C=C5)O)C(=N)O)O)O)CC6=CC=CC=C6)O)C)O)CC(=N)O)O)CC7=CNC8=CC=CC=C87)O
CHEMBL347216 mshr_mouse Mouse No 6.9 EC50 = 127 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
697 18 8 7 1.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)N
CHEMBL3577993 mshr_mouse Mouse No 4.9 EC50 = 12700 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC5=CC=CC=C54)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3577993 mshr_mouse Mouse No 4.9 EC50 = 12700 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC5=CC=CC=C54)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL439361 mshr_human Human No 5.9 EC50 = 1275 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1033 15 11 10 2.6 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(CCC3=C(C2)C=CC=C3OCC)NC1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL439361 mshr_human Human No 5.9 EC50 = 1275 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1033 15 11 10 2.6 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(CCC3=C(C2)C=CC=C3OCC)NC1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL183733 mshr_human Human No 7.9 EC50 = 13 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
833 22 10 8 1.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL3646891 mshr_human Human No 7.9 EC50 = 13 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1044 18 15 12 -3.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCC(=O)NCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL183733 mshr_human Human No 7.9 EC50 = 13 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
833 22 10 8 1.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL50056 mshr_human Human Yes 7.9 EC50 = 13 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL410217 mshr_human Human No 7.9 EC50 = 13.4 Funct
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor
982 12 13 11 -1.4 CC1C(=O)NC(CCCCNC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C)C(=O)N
CHEMBL88537 mshr_human Human No 7.9 EC50 = 13.7 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
730 21 10 8 -0.4 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)CCCO
CHEMBL2371967 mshr_human Human No 6.9 EC50 = 130 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
1077 12 8 9 5.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCCN2C(=O)C(NC(=O)C3CC4=CC=CC=C4CN3C1=O)CC5=CC=C(C=C5)C6=CC=CC=C6)CC7=CNC8=CC=CC=C87)C(=O)N)NC(=O)C
CHEMBL2371967 mshr_human Human No 6.9 EC50 = 130 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
1077 12 8 9 5.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCCN2C(=O)C(NC(=O)C3CC4=CC=CC=C4CN3C1=O)CC5=CC=C(C=C5)C6=CC=CC=C6)CC7=CNC8=CC=CC=C87)C(=O)N)NC(=O)C
CHEMBL203911 mshr_human Human No 5.9 EC50 = 1300 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
621 8 2 5 6.3 CC1COC(=O)N1CC2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)C6CCCCC6
CHEMBL265985 mshr_human Human No 5.9 EC50 = 1300 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
607 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6CCOC6=O
CHEMBL389674 mshr_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
965 13 10 10 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CC5=CC6=CC=CC=C6N5)C(=O)N)NC(=O)C
CHEMBL199037 mshr_human Human No 5.9 EC50 = 1300 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
792 20 8 6 4.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL197695 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
849 22 9 7 3.4 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL382511 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
849 22 9 7 3.4 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL199037 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
792 20 8 6 4.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL436329 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
865 22 10 8 3.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=C(C=C2)O)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL203911 mshr_human Human No 5.9 EC50 = 1300 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
621 8 2 5 6.3 CC1COC(=O)N1CC2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)C6CCCCC6
CHEMBL265985 mshr_human Human No 5.9 EC50 = 1300 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
607 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6CCOC6=O
CHEMBL389674 mshr_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
965 13 10 10 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC=CC=C4)CC5=CC6=CC=CC=C6N5)C(=O)N)NC(=O)C
CHEMBL199037 mshr_human Human No 5.9 EC50 = 1300 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
792 20 8 6 4.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL197695 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
849 22 9 7 3.4 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL382511 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
849 22 9 7 3.4 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL199037 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
792 20 8 6 4.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=CC=C2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL436329 mshr_human Human No 5.9 EC50 = 1300 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
865 22 10 8 3.0 CCCCC(=O)NC1(CCC(CC1)C2=CC=C(C=C2)O)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL379627 mshr_human Human Yes 5.9 EC50 = 1303.7 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
740 10 9 7 1.2 C1CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL379627 mshr_human Human Yes 5.9 EC50 = 1303.7 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
740 10 9 7 1.2 C1CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL437822 mshr_human Human No 5.9 EC50 = 1330 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1047 15 11 10 3.0 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(CCC3=C(C2)C=CC=C3OC(C)C)NC1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL437822 mshr_human Human No 5.9 EC50 = 1330 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1047 15 11 10 3.0 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(CCC3=C(C2)C=CC=C3OC(C)C)NC1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL2371699 mshr_mouse Mouse No 4.9 EC50 = 13300 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1490 24 21 22 -3.3 CC1C(=O)NC(C(=O)NC(NC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC=N4)NNC5CC6=C(C=C(C=C6)O)NC5=O)C(=O)NNC(CC7=CC=C(C=C7)O)C(=O)C(=O)O)CC8=CC=CC=C8
CHEMBL375559 mshr_human Human No 5.9 EC50 = 1337 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
708 15 6 7 2.7 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL375559 mshr_human Human No 5.9 EC50 = 1337 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
708 15 6 7 2.7 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL3143817 mshr_human Human No 6.9 EC50 = 135 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
698 10 9 7 0.1 C1CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54
CHEMBL3143817 mshr_human Human No 6.9 EC50 = 135 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
698 10 9 7 0.1 C1CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54
CHEMBL413465 mshr_mouse Mouse No 4.9 EC50 = 13500 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1421 24 20 21 -2.4 CC1C(=O)NC(C(=O)C(=O)NC(NC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CC=C(C=C5)O)NN)C(=O)NNC(CC6=CC=C(C=C6)O)C(=O)C(=O)O)CC7=CC=CC=C7
CHEMBL3577984 mshr_mouse Mouse No 4.9 EC50 = 13600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
963 11 9 10 0.3 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)C5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL3577984 mshr_mouse Mouse No 4.9 EC50 = 13600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
963 11 9 10 0.3 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)C5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL210008 mshr_human Human No 5.9 EC50 = 1362 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
633 12 4 5 4.3 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C3CC4=CC=CC=C4CN3)OCC5=CC6=CC=CC=C6C=C5
CHEMBL210008 mshr_human Human No 5.9 EC50 = 1362 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
633 12 4 5 4.3 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C3CC4=CC=CC=C4CN3)OCC5=CC6=CC=CC=C6C=C5
CHEMBL591041 mshr_human Human No 5.9 EC50 = 1380.4 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
568 9 1 6 4.0 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)C5=CC=CC=C5
CHEMBL591041 mshr_human Human No 5.9 EC50 = 1380.4 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
568 9 1 6 4.0 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)C5=CC=CC=C5
CHEMBL3798912 mshr_mouse Mouse No 6.9 EC50 = 139 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1012 35 11 13 -0.2 C1=CC=C2C=C(C=CC2=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C(CC5=CN=CN5)NC(=O)COCC(=O)NCCCOCCOCCOCCCN
CHEMBL3798912 mshr_mouse Mouse No 6.9 EC50 = 139 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1012 35 11 13 -0.2 C1=CC=C2C=C(C=CC2=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)NC(=O)C(CC5=CN=CN5)NC(=O)COCC(=O)NCCCOCCOCCOCCCN
CHEMBL215576 mshr_human Human No 5.9 EC50 = 1391 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
561 11 3 5 2.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)N3CCN(C(C3=O)CCCN=C(N)N)C(=O)CCC4=CC=C(C=C4)F
CHEMBL215576 mshr_human Human No 5.9 EC50 = 1391 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
561 11 3 5 2.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)N3CCN(C(C3=O)CCCN=C(N)N)C(=O)CCC4=CC=C(C=C4)F
CHEMBL211699 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
711 18 8 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL211699 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
711 18 8 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL50056 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2112920 mshr_human Human No 7.9 EC50 = 14 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
782 22 9 8 1.3 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCC(=O)N
CHEMBL3646885 mshr_human Human No 7.9 EC50 = 14 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1044 18 15 12 -3.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCCCNC(=O)CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL211699 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
711 18 8 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL211699 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
711 18 8 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL50056 mshr_human Human Yes 7.9 EC50 = 14 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2323786 mshr_mouse Mouse Yes 7.9 EC50 = 14 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1647 24 19 21 1.8 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CCCNC(=N)N)C(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CC4=CC=CC=C4C=C3)CC5=CC=CC=C5)CC6=CNC=N6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL2112920 mshr_human Human No 7.9 EC50 = 14 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
782 22 9 8 1.3 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCC(=O)N
CHEMBL2112920 mshr_human Human No 7.9 EC50 = 14 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
782 22 9 8 1.3 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCC(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.9 EC50 = 14.1 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.9 EC50 = 14.1 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL598617 mshr_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
544 7 1 6 4.4 CC(C)N(C1=CC=C(C=C1)F)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL598617 mshr_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
544 7 1 6 4.4 CC(C)N(C1=CC=C(C=C1)F)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL3600736 mshr_human Human No 7.8 EC50 = 14.8 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600736 mshr_human Human No 7.8 EC50 = 14.8 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1074 17 13 11 1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL501394 mshr_mouse Mouse Yes 6.9 EC50 = 140 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
755 18 9 7 1.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC(=C(C=C2)Cl)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 6.9 EC50 = 140 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL412174 mshr_human Human No 6.9 EC50 = 140 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
1068 13 11 9 3.0 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2(CCC3=C(C2)C=C(C=C3)Br)NC1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL501394 mshr_mouse Mouse Yes 6.9 EC50 = 140 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
755 18 9 7 1.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC(=C(C=C2)Cl)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL510270 mshr_human Human Yes 5.9 EC50 = 1400 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1592 46 22 19 0.7 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)N)NC(=N)N)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)C
CHEMBL510270 mshr_human Human Yes 5.9 EC50 = 1400 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1592 46 22 19 0.7 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)N)NC(=N)N)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)C
CHEMBL339053 mshr_human Human Yes 5.9 EC50 = 1400 Funct
In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 1 receptor (hMC1R)In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 1 receptor (hMC1R)
589 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C=NC=N6
CHEMBL2369968 mshr_mouse Mouse No 4.9 EC50 = 14000 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1411 21 19 19 -4.4 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)N1)CC2=CNC=N2)NC(=O)C(CC3=CC=C(C=C3)O)N)C(CC4=CC=C(C=C4)O)C(=O)N)(C)C(=O)O)CC5=CC=CC=C5)C)CC(=O)N)CC6=CNC7=CC=CC=C76)CCCN=C(N)N
CHEMBL2369968 mshr_mouse Mouse No 4.9 EC50 = 14000 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1411 21 19 19 -4.4 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)N1)CC2=CNC=N2)NC(=O)C(CC3=CC=C(C=C3)O)N)C(CC4=CC=C(C=C4)O)C(=O)N)(C)C(=O)O)CC5=CC=CC=C5)C)CC(=O)N)CC6=CNC7=CC=CC=C76)CCCN=C(N)N
CHEMBL302703 mshr_human Human No 5.9 EC50 = 1428 Funct
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL187125 mshr_human Human No 5.8 EC50 = 1430 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
754 19 8 7 4.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC5=CC=CO5
CHEMBL187125 mshr_human Human No 5.9 EC50 = 1430 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
754 19 8 7 4.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC5=CC=CO5
CHEMBL365044 mshr_human Human No 6.8 EC50 = 144 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
848 23 8 6 4.9 C1=CC=C(C=C1)CCCCC(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL365044 mshr_human Human No 6.8 EC50 = 144 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
848 23 8 6 4.9 C1=CC=C(C=C1)CCCCC(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL453734 mshr_human Human No 6.8 EC50 = 145 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
604 11 3 6 4.0 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C(C)(C)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL453734 mshr_human Human No 6.8 EC50 = 145 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
604 11 3 6 4.0 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C(C)(C)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL302703 mshr_mouse Mouse No 4.8 EC50 = 14500 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2373991 mshr_mouse Mouse No 5.8 EC50 = 1460 Funct
Agonistic activity against mouse Melanocortin 1 ReceptorAgonistic activity against mouse Melanocortin 1 Receptor
2573 39 32 37 -5.8 CCC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC2CSSCC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N3CCCC3C(=O)N1)CC(=O)O)CC)N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)O)CC4=CC=C(C=C4)O)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CCCN=C(N)N)CC5=CC=CC=C5)CC6=CC=CC=C6)CC(=O)N)C)CC7=CC=CC=C7)CC8=CC=C(C=C8)O)CC)C(C)O)C
CHEMBL2373991 mshr_mouse Mouse No 5.8 EC50 = 1460 Funct
Agonistic activity against mouse Melanocortin 1 ReceptorAgonistic activity against mouse Melanocortin 1 Receptor
2573 39 32 37 -5.8 CCC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC2CSSCC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)N3CCCC3C(=O)N1)CC(=O)O)CC)N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)O)CC4=CC=C(C=C4)O)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CCCN=C(N)N)CC5=CC=CC=C5)CC6=CC=CC=C6)CC(=O)N)C)CC7=CC=CC=C7)CC8=CC=C(C=C8)O)CC)C(C)O)C
CHEMBL317228 mshr_mouse Mouse No 4.8 EC50 = 14700 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
672 17 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(C2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL29693 mshr_human Human No 5.8 EC50 = 1480 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
851 22 9 8 2.7 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2OC)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL305391 mshr_mouse Mouse No 4.8 EC50 = 14800 Funct
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cellsAgonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
422 11 5 3 2.3 C1=CC=C(C=C1)CNC(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NCCCCCN
CHEMBL2323799 mshr_mouse Mouse Yes 7.8 EC50 = 15 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1650 25 20 21 1.0 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CCCCNC(=N)N)C(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CNC4=CC=CC=C43)CC5=CC=CC=C5)CC6=CNC=N6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL311750 mshr_human Human No 7.8 EC50 = 15 Funct
Agonist potency for human Melanocortin 1 receptorAgonist potency for human Melanocortin 1 receptor
782 24 10 9 1.3 CCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)NC#N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL598011 mshr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL598011 mshr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL2373212 mshr_human Human No 6.8 EC50 = 150 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
782 22 9 8 1.3 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=CC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL381125 mshr_human Human No 5.8 EC50 = 1500 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
657 10 2 6 6.3 CC(C)N(CC1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)Cl)NC(=O)C3CC4=CC=CC=C4CN3)C5CCCCC5)S(=O)(=O)C
CHEMBL3577985 mshr_mouse Mouse No 5.8 EC50 = 1500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
991 13 9 10 1.0 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CCC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL381125 mshr_human Human No 5.8 EC50 = 1500 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
657 10 2 6 6.3 CC(C)N(CC1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)Cl)NC(=O)C3CC4=CC=CC=C4CN3)C5CCCCC5)S(=O)(=O)C
CHEMBL2096745 mshr_mouse Mouse No 5.8 EC50 = 1500 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
659 15 7 7 -0.4 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)N3CC4=CC=CC=C4CC3C(=O)N
CHEMBL3577985 mshr_mouse Mouse No 5.8 EC50 = 1500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
991 13 9 10 1.0 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CCC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL106959 mshr_mouse Mouse No 5.8 EC50 = 1500 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
762 19 9 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL460138 mshr_human Human No 5.8 EC50 = 1505 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
519 9 2 5 4.1 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL460138 mshr_human Human No 5.8 EC50 = 1505 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
519 9 2 5 4.1 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL379879 mshr_human Human No 6.8 EC50 = 151 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
474 10 3 4 2.8 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)N)OCC3=CC4=CC=CC=C4C=C3
CHEMBL379879 mshr_human Human No 6.8 EC50 = 151 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
474 10 3 4 2.8 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)N)OCC3=CC4=CC=CC=C4C=C3
CHEMBL319922 mshr_mouse Mouse No 4.8 EC50 = 15200 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
736 18 9 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC3=CC=CC=C32)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL460142 mshr_human Human No 5.8 EC50 = 1523 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
519 8 2 5 4.2 CC(C)C1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL460142 mshr_human Human No 5.8 EC50 = 1523 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
519 8 2 5 4.2 CC(C)C1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL598010 mshr_human Human No 5.8 EC50 = 1548.8 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL598010 mshr_human Human No 5.8 EC50 = 1548.8 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL3600840 mshr_human Human No 5.8 EC50 = 1560 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600840 mshr_human Human No 5.8 EC50 = 1560 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL1682209 mshr_human Human No 7.8 EC50 = 16 Funct
Agonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation
644 11 2 8 3.6 COCC(=O)NC1CC2=CC(=C(C=C2)OC)CC3=CC=C(C=C3)OC4=CC=CC(=C4)CN(C1=O)CCCN5CCN(CC5)CCCN
CHEMBL1682209 mshr_human Human No 7.8 EC50 = 16 Funct
Agonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC1 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation
644 11 2 8 3.6 COCC(=O)NC1CC2=CC(=C(C=C2)OC)CC3=CC=C(C=C3)OC4=CC=CC(=C4)CN(C1=O)CCCN5CCN(CC5)CCCN
CHEMBL2323800 mshr_mouse Mouse No 7.8 EC50 = 16 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1548 19 16 20 1.8 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC2CSCC(=O)C3(CCCN3C2=O)C(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CC6=CC=CC=C6)CC7=CN=CN7)NC(=O)C(CC8=CC=C(C=C8)O)N)C(=O)NC(CC9=CC=C(C=C9)O)C(=O)N)CC1=CC=CC=C1
CHEMBL3799094 mshr_mouse Mouse No 7.8 EC50 = 16.4 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1569 37 17 19 -3.2 C1CC(NC1)C(=O)NCC(=O)N2CCCC2C(=O)NCC(=O)N3CCCC3C(=O)NCC(=O)N4CCCC4C(=O)NCC(=O)N5CCCC5C(=O)NCC(=O)N6CCCC6C(=O)NCC(=O)NC(CC7=CN=CN7)C(=O)NC(CC8=CC=CC=C8)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC9=CNC1=CC=CC=C19)C(=O)N
CHEMBL3799094 mshr_mouse Mouse No 7.8 EC50 = 16.4 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1569 37 17 19 -3.2 C1CC(NC1)C(=O)NCC(=O)N2CCCC2C(=O)NCC(=O)N3CCCC3C(=O)NCC(=O)N4CCCC4C(=O)NCC(=O)N5CCCC5C(=O)NCC(=O)N6CCCC6C(=O)NCC(=O)NC(CC7=CN=CN7)C(=O)NC(CC8=CC=CC=C8)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC9=CNC1=CC=CC=C19)C(=O)N
CHEMBL194552 mshr_human Human Yes 6.8 EC50 = 160 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1015 13 10 10 2.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC5=CC=CC=C5C=C4)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL194552 mshr_human Human Yes 6.8 EC50 = 160 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1015 13 10 10 2.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC5=CC=CC=C5C=C4)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL272662 mshr_mouse Mouse No 4.8 EC50 = 16450 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
365 6 3 3 1.1 C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=O)NC(C2=O)CCCN=C(N)N
CHEMBL272662 mshr_mouse Mouse No 4.8 EC50 = 16450 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
365 6 3 3 1.1 C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=O)NC(C2=O)CCCN=C(N)N
CHEMBL103817 mshr_mouse Mouse No 6.8 EC50 = 167 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
736 18 9 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL569104 mshr_mouse Mouse No 5.8 EC50 = 1670 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
591 17 7 7 -0.6 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CN=CC=C3
CHEMBL569104 mshr_mouse Mouse No 5.8 EC50 = 1670 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
591 17 7 7 -0.6 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC3=CN=CC=C3
CHEMBL566545 mshr_mouse Mouse No 5.8 EC50 = 1690 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
618 17 7 7 0.6 COC1=CC=CC=C1C=CC(=O)NC(CC2=CN=CN2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)N
CHEMBL566545 mshr_mouse Mouse No 5.8 EC50 = 1690 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
618 17 7 7 0.6 COC1=CC=CC=C1C=CC(=O)NC(CC2=CN=CN2)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)N
CHEMBL318119 mshr_mouse Mouse No 4.8 EC50 = 16900 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
672 17 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(C2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL460349 mshr_human Human No 5.8 EC50 = 1697 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
505 8 2 5 3.7 CCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL460349 mshr_human Human No 5.8 EC50 = 1697 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
505 8 2 5 3.7 CCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL357558 mshr_mouse Mouse No 7.8 EC50 = 17.9 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
697 18 8 7 1.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)N
CHEMBL442829 mshr_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
616 11 3 6 4.5 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCCN3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL503449 mshr_mouse Mouse No 6.8 EC50 = 170 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
700 18 9 7 0.4 CC1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)C
CHEMBL442829 mshr_human Human No 6.8 EC50 = 170 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
616 11 3 6 4.5 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3CCCN3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL503449 mshr_mouse Mouse No 6.8 EC50 = 170 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
700 18 9 7 0.4 CC1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)C
CHEMBL343094 mshr_mouse Mouse No 6.8 EC50 = 170 Funct
Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells
686 18 8 7 -0.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N(CCCN=C(N)N)CC(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL380635 mshr_human Human No 5.8 EC50 = 1700 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
647 8 2 5 6.6 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C(=O)OCC67CCC7
CHEMBL502300 mshr_human Human No 5.8 EC50 = 1700 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1091 16 13 11 -0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CC(CN2C1=O)N=C(N)N)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL380635 mshr_human Human No 5.8 EC50 = 1700 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
647 8 2 5 6.6 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C(=O)OCC67CCC7
CHEMBL502300 mshr_human Human No 5.8 EC50 = 1700 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1091 16 13 11 -0.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CC(CN2C1=O)N=C(N)N)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL309213 mshr_human Human No 5.8 EC50 = 1700 Funct
Agonist potency for human Melanocortin 1 receptorAgonist potency for human Melanocortin 1 receptor
738 21 9 8 1.5 CCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CC3=CN=CN3)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL140847 mshr_mouse Mouse No 5.8 EC50 = 1700 Funct
Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells
700 19 8 7 0.1 CC(=O)N(CCC1=CN=CN1)CC(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL2370695 mshr_mouse Mouse No 5.8 EC50 = 1730 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1310 21 17 17 -2.5 CC1C(=O)NC(C(=O)NC(CNC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)NC(=O)C(CC4=CC=C(C=C4)O)N)C(=O)NC(CC5=CC=C(C=C5)O)C(=O)O)CC6=CC=CC=C6
CHEMBL569221 mshr_mouse Mouse No 5.8 EC50 = 1745 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
618 18 7 7 -0.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC(=O)C3=CC=CC=C3
CHEMBL569221 mshr_mouse Mouse No 5.8 EC50 = 1745 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
618 18 7 7 -0.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)CCC(=O)C3=CC=CC=C3
CHEMBL2304248 mshr_mouse Mouse No 5.8 EC50 = 1750 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
2327 55 32 33 -6.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCNC(=N)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C)NC(=O)C5CCCN5C(=O)C(CC(=O)O)N)C(=O)NC(CC6=CC=C(C=C6)O)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)O)CC7=CC=CC=C7
CHEMBL2304248 mshr_mouse Mouse No 5.8 EC50 = 1750 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
2327 55 32 33 -6.4 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCNC(=N)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C)NC(=O)C5CCCN5C(=O)C(CC(=O)O)N)C(=O)NC(CC6=CC=C(C=C6)O)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)O)CC7=CC=CC=C7
CHEMBL213026 mshr_human Human No 5.8 EC50 = 1751 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
679 15 5 6 4.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL213026 mshr_human Human No 5.8 EC50 = 1751 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
679 15 5 6 4.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL317968 mshr_mouse Mouse No 6.8 EC50 = 176 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
697 18 8 7 0.5 CC(=O)NC(CC1=CC=NC=C1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3577979 mshr_mouse Mouse No 4.8 EC50 = 17600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1446 17 16 16 2.5 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)N1)CC4=CC=C(C=C4)O)CC5=CC=C(C=C5)O)C)CC6=CC=CC=C6)C)CC(=O)N)CC7=CC=CC=C7)CC8=CC=CC=C8)CCCNC(=N)N
CHEMBL3577979 mshr_mouse Mouse No 4.8 EC50 = 17600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1446 17 16 16 2.5 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)N1)CC4=CC=C(C=C4)O)CC5=CC=C(C=C5)O)C)CC6=CC=CC=C6)C)CC(=O)N)CC7=CC=CC=C7)CC8=CC=CC=C8)CCCNC(=N)N
CHEMBL604911 mshr_human Human No 6.8 EC50 = 177.8 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
539 8 1 6 3.1 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CN=CC=C5
CHEMBL604911 mshr_human Human No 6.8 EC50 = 177.8 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
539 8 1 6 3.1 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CN=CC=C5
CHEMBL264190 mshr_mouse Mouse Yes 7.8 EC50 = 18 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3646882 mshr_human Human No 7.8 EC50 = 18 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1058 19 15 12 -3.5 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCCNC(=O)CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3646890 mshr_human Human No 7.8 EC50 = 18 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1044 18 15 12 -3.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCCC(=O)NCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.8 EC50 = 18 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL455826 mshr_mouse Mouse No 6.8 EC50 = 180 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
776 20 9 7 1.9 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL455826 mshr_mouse Mouse No 6.8 EC50 = 180 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
776 20 9 7 1.9 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL347864 mshr_human Human No 6.8 EC50 = 180 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
787 22 11 9 -0.2 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL272439 mshr_mouse Mouse No 5.8 EC50 = 1800 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
400 6 3 3 1.7 C1=CC=C(C=C1)CN2C3=C(C=CC(=C3)Cl)C(=O)NC(C2=O)CCCN=C(N)N
CHEMBL272439 mshr_mouse Mouse No 5.8 EC50 = 1800 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
400 6 3 3 1.7 C1=CC=C(C=C1)CN2C3=C(C=CC(=C3)Cl)C(=O)NC(C2=O)CCCN=C(N)N
CHEMBL330233 mshr_mouse Mouse No 5.8 EC50 = 1800 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
620 16 8 6 -0.2 CC(C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C
CHEMBL379490 mshr_human Human No 5.7 EC50 = 1815 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
679 15 5 6 4.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL379490 mshr_human Human No 5.7 EC50 = 1815 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
679 15 5 6 4.1 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL1089461 mshr_human Human No 5.7 EC50 = 1850 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
494 4 1 8 2.5 CC1CN(CC(C1(C2=CC=CC=N2)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C5=NN=CC=C5
CHEMBL1089461 mshr_human Human No 5.7 EC50 = 1850 Funct
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assayAgonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
494 4 1 8 2.5 CC1CN(CC(C1(C2=CC=CC=N2)O)C)C(=O)C3CN(CC3C4=C(C=C(C=C4)F)F)C5=NN=CC=C5
CHEMBL598021 mshr_human Human No 6.7 EC50 = 186.2 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
526 7 1 5 4.3 CC(C)N(C1=CC=CC=C1)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL598021 mshr_human Human No 6.7 EC50 = 186.2 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
526 7 1 5 4.3 CC(C)N(C1=CC=CC=C1)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC(=CC4=NN3)F)C5=CC=CC=C5
CHEMBL184326 mshr_human Human No 5.7 EC50 = 1894 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
812 21 8 9 3.9 COP(=S)(NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)OC
CHEMBL184326 mshr_human Human No 5.7 EC50 = 1894 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
812 21 8 9 3.9 COP(=S)(NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N)OC
CHEMBL213751 mshr_human Human No 7.7 EC50 = 19 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
633 12 4 5 4.3 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C3CC4=CC=CC=C4CN3)OCC5=CC6=CC=CC=C6C=C5
CHEMBL3287327 mshr_mouse Mouse No 7.7 EC50 = 19 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
807 18 8 7 1.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)N
CHEMBL213751 mshr_human Human No 7.7 EC50 = 19 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
633 12 4 5 4.3 C1C(CN(C1CCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C3CC4=CC=CC=C4CN3)OCC5=CC6=CC=CC=C6C=C5
CHEMBL2323797 mshr_mouse Mouse Yes 7.7 EC50 = 19 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1551 19 19 32 6.4 CC1CN2C(C(=NC(C(=NC(C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC(CSCC2=O)C(=N1)O)O)CC3=CC=CC=C3)O)CC4=CN=CN4)O)N=C(C(CC5=CC=C(C=C5)O)N)O)C(=NC(CC6=CC=C(C=C6)O)C(=N)O)O)O)CC7=CC=CC=C7)O)C)O)CC(=N)O)O)CC8=CNC9=CC=CC=C98
CHEMBL3287327 mshr_mouse Mouse No 7.7 EC50 = 19 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
807 18 8 7 1.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)N
CHEMBL1688104 mshr_mouse Mouse Yes 6.7 EC50 = 190 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CNC=N3)C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CC=CC=C6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL1688104 mshr_mouse Mouse Yes 6.7 EC50 = 190 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CNC=N3)C(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CC=CC=C6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL508501 mshr_human Human No 4.7 EC50 = 19000 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1072 14 12 11 0.9 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CC(CN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC5=CC=CC=C5C=C4)N=C(N)N)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL508501 mshr_human Human No 4.7 EC50 = 19000 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1072 14 12 11 0.9 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CC(CN2C(=O)C(NC(=O)C(NC1=O)CC3=CN=CN3)CC4=CC5=CC=CC=C5C=C4)N=C(N)N)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL432018 mshr_mouse Mouse No 4.7 EC50 = 19000 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
762 19 9 7 1.5 CC(=O)NC(CC1=CN=CN1)C(=O)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL463047 mshr_human Human No 6.7 EC50 = 193 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
624 11 2 6 4.9 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3=CN=CC=C3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL463047 mshr_human Human No 6.7 EC50 = 193 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
624 11 2 6 4.9 CCCC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)NC(=O)C3=CN=CC=C3)C(CC4=CC5=CC=CC=C5C=C4)C(=O)NC
CHEMBL282533 mshr_human Human No 6.7 EC50 = 195 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
849 22 9 7 3.5 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2CC)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL3577994 mshr_mouse Mouse No 4.7 EC50 = 19600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC5=CC=CC=C5C=C4)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3577994 mshr_mouse Mouse No 4.7 EC50 = 19600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC5=CC=CC=C5C=C4)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3600921 mshr_human Human No 5.7 EC50 = 1970 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600921 mshr_human Human No 5.7 EC50 = 1970 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL440633 mshr_mouse Mouse No 4.7 EC50 = 19700 Funct
Effective concentration against mouse Melanocortin 1 receptorEffective concentration against mouse Melanocortin 1 receptor
1421 24 20 21 -2.4 CC1C(=O)NC(C(=O)C(=O)NC(NC(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)NC(=O)C(CC5=CC=C(C=C5)O)NN)C(=O)NNC(CC6=CC=C(C=C6)O)C(=O)C(=O)O)CC7=CC=CC=C7
CHEMBL183476 mshr_human Human No 5.7 EC50 = 1982 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
744 19 8 6 2.6 CCC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL183476 mshr_human Human No 5.7 EC50 = 1982 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
744 19 8 6 2.6 CCC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL504986 mshr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulation
894 11 10 11 1.2 C1C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2=C(S1)C=CC(=C2)[N+](=O)[O-])CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL504986 mshr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as cAMP accumulation
894 11 10 11 1.2 C1C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2=C(S1)C=CC(=C2)[N+](=O)[O-])CC3=CN=CN3)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL269338 mshr_human Human No 8.7 EC50 = 2 Funct
Agonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assayAgonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assay
1131 19 14 12 0.7 CC(C)C(C(=O)NC(C(C)C)C(=O)NCC(=O)N)NC(=O)C1CCC(=O)NCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC5=CC=CC=C5C=C4)CC6=CN=CN6
CHEMBL2114258 mshr_human Human No 8.7 EC50 = 2 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)C(C)C3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL2371712 mshr_human Human No 8.7 EC50 = 2 Funct
Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)
1589 45 18 20 0.9 CCCCC(C(=O)NCC(=O)N1CCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NC(CC(=O)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)ON)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)N
CHEMBL438920 mshr_human Human No 8.7 EC50 = 2 Funct
Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)
1579 48 20 21 -0.9 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC(CC(=O)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC5=CC=CC=C5)C(=O)NCC(=O)ON)NC(=O)C(C(C)C)NC(=O)C(CC6=CC=C(C=C6)O)N
CHEMBL413212 mshr_human Human No 8.7 EC50 = 2 Funct
Evaluated for agonist at cloned mammalian Melanocortin 1 receptor in frog (Rana pipiens) skin assayEvaluated for agonist at cloned mammalian Melanocortin 1 receptor in frog (Rana pipiens) skin assay
1059 17 13 11 0.7 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=C(C=C3)Cl)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL406276 mshr_human Human No 8.7 EC50 = 2 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
728 21 9 7 1.4 CCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL419307 mshr_human Human No 8.7 EC50 = 2 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
812 21 9 8 2.3 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)COC5=CC=C(C=C5)Cl
CHEMBL89004 mshr_human Human No 8.7 EC50 = 2 Funct
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
762 20 9 7 1.6 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)CC5=CC=CC=C5
CHEMBL193151 mshr_mouse Mouse No 8.7 EC50 = 2.1 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
868 31 9 7 6.8 CCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL193151 mshr_mouse Mouse No 8.7 EC50 = 2.1 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
868 31 9 7 6.8 CCCCCCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3600837 mshr_human Human No 8.7 EC50 = 2.1 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL3600837 mshr_human Human No 8.7 EC50 = 2.1 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL384176 mshr_human Human No 8.6 EC50 = 2.3 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
618 12 4 6 2.3 CC(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCN(C(=O)C2CCCN=C(N)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL384176 mshr_human Human No 8.6 EC50 = 2.3 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
618 12 4 6 2.3 CC(=O)NC(CC1=CC=C(C=C1)F)C(=O)N2CCN(C(=O)C2CCCN=C(N)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL1688111 mshr_mouse Mouse Yes 8.6 EC50 = 2.4 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1636 24 22 33 5.6 CC1C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=N1)O)CC(=N)O)O)CC3=CNC4=CC=CC=C43)O)CC5=CC=CC=C5)O)CC6=CN=CN6)O)N=C(C(CC7=CC=C(C=C7)O)N)O)C(=NC(CC8=CC=C(C=C8)O)C(=N)O)O)O)CC9=CC=CC=C9)O
CHEMBL276301 mshr_human Human No 8.6 EC50 = 2.5 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
531 12 2 5 3.6 CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)CCC3=CN=CN3)C4=CC=CC=C4
CHEMBL2369983 mshr_mouse Mouse No 8.6 EC50 = 2.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1487 23 19 19 -2.8 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL217584 mshr_human Human No 8.6 EC50 = 2.6 Funct
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor
1095 17 14 12 -0.2 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C)C(=O)N)NC(=O)C
CHEMBL2369983 mshr_mouse Mouse No 8.6 EC50 = 2.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1487 23 19 19 -2.8 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL3287324 mshr_mouse Mouse No 8.6 EC50 = 2.7 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
840 15 6 8 1.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)I)C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(CC4=CC=C(C=C4)[N+](=O)[O-])C(=O)N
CHEMBL3287324 mshr_mouse Mouse No 8.6 EC50 = 2.7 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
840 15 6 8 1.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)I)C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(CC4=CC=C(C=C4)[N+](=O)[O-])C(=O)N
CHEMBL194217 mshr_mouse Mouse No 8.6 EC50 = 2.8 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
812 27 9 7 4.6 CCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL194217 mshr_mouse Mouse No 8.6 EC50 = 2.8 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
812 27 9 7 4.6 CCCCCCCCCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3287322 mshr_mouse Mouse No 8.5 EC50 = 2.9 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
821 13 5 8 2.9 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)N3CC4=CC=CC=C4CC3C(=O)NC(CC5=CC=C(C=C5)[N+](=O)[O-])C(=O)N
CHEMBL3287322 mshr_mouse Mouse No 8.5 EC50 = 2.9 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
821 13 5 8 2.9 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)N3CC4=CC=CC=C4CC3C(=O)NC(CC5=CC=C(C=C5)[N+](=O)[O-])C(=O)N
CHEMBL3601428 mshr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL264190 mshr_mouse Mouse Yes 7.7 EC50 = 20 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3601428 mshr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL2323787 mshr_mouse Mouse Yes 7.7 EC50 = 20 Funct
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
1673 25 21 33 7.1 CC1C(=NC(C(=NC(CSSCC(C(=NC(C(=NC(C(=NC2CSCC(=O)N(CC(N=C2O)CCCNC(=N)N)C(C(=NC(C(=N1)O)CC(=N)O)O)CC3=CC=C(C=C3)C4=CC=CC=C4)O)CC5=CC=CC=C5)O)CC6=CN=CN6)O)N=C(C(CC7=CC=C(C=C7)O)N)O)C(=NC(CC8=CC=C(C=C8)O)C(=N)O)O)O)CC9=CC=CC=C9)O
CHEMBL264190 mshr_mouse Mouse Yes 7.7 EC50 = 20 Funct
Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL348511 mshr_human Human No 7.7 EC50 = 20 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
805 22 10 8 0.8 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL152612 mshr_mouse Mouse No 7.7 EC50 = 20.1 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.7 EC50 = 20.1 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.7 EC50 = 20.1 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL272099 mshr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cellsAgonist activity at human MC1 receptor expressed in HEK293 cells
430 6 1 4 4.5 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)N)CN4C=NC=N4
CHEMBL3422427 mshr_mouse Mouse No 5.7 EC50 = 2000 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
861 18 9 6 2.6 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL272099 mshr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cellsAgonist activity at human MC1 receptor expressed in HEK293 cells
430 6 1 4 4.5 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)N)CN4C=NC=N4
CHEMBL3422427 mshr_mouse Mouse No 5.7 EC50 = 2000 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
861 18 9 6 2.6 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL202699 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
737 18 8 7 3.0 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL387246 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
532 13 6 5 1.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)N
CHEMBL202699 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
737 18 8 7 3.0 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL387246 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
532 13 6 5 1.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)N
CHEMBL202699 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
737 18 8 7 3.0 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL387246 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
532 13 6 5 1.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)N
CHEMBL202699 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
737 18 8 7 3.0 CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL387246 mshr_human Human Yes 4.7 EC50 = 20000 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
532 13 6 5 1.8 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=CC=C3)N
CHEMBL63850 mshr_mouse Mouse No 4.7 EC50 = 20000 Funct
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cellsAgonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
491 11 5 4 2.7 C1CN(CCC1CC2=CC=CC=C2)NC(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCCCCN
CHEMBL378446 mshr_human Human No 6.7 EC50 = 201 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
663 15 4 5 4.4 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL378446 mshr_human Human No 6.7 EC50 = 201 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
663 15 4 5 4.4 CC(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL330561 mshr_mouse Mouse No 6.7 EC50 = 203 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
702 18 8 7 1.2 CC(=O)NC(CC1=CC=CS1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3577991 mshr_mouse Mouse No 4.7 EC50 = 20300 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
991 13 9 10 1.0 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CCC4=CC=CC=C4)CC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL3577991 mshr_mouse Mouse No 4.7 EC50 = 20300 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
991 13 9 10 1.0 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CCC4=CC=CC=C4)CC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL63867 mshr_mouse Mouse No 4.7 EC50 = 20500 Funct
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cellsAgonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
475 13 4 4 3.4 C1=CC=C(C=C1)CNC(=O)NC(CC2=CC=C(C=C2)OCC3=CC=CC=C3)C(=O)NCCCCN
CHEMBL565900 mshr_mouse Mouse No 5.7 EC50 = 2060 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
629 16 8 8 0.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C(=CC3=CC=C(C=C3)O)C#N
CHEMBL565900 mshr_mouse Mouse No 5.7 EC50 = 2060 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
629 16 8 8 0.2 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C(=CC3=CC=C(C=C3)O)C#N
CHEMBL3422428 mshr_mouse Mouse No 4.7 EC50 = 20700 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
898 19 8 6 3.8 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC=C(C=C4)C5=CC=CC=C5)C(=O)N
CHEMBL3422428 mshr_mouse Mouse No 4.7 EC50 = 20700 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
898 19 8 6 3.8 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC=C(C=C4)C5=CC=CC=C5)C(=O)N
CHEMBL2369966 mshr_mouse Mouse No 7.7 EC50 = 21.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1460 21 17 19 -3.1 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(C(=O)N1)CC(=O)N)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369966 mshr_mouse Mouse No 7.7 EC50 = 21.6 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1460 21 17 19 -3.1 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(C(=O)N1)CC(=O)N)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CNC=N5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL372274 mshr_human Human No 6.7 EC50 = 210 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
933 26 9 7 6.0 CCCCC(=O)NC1(CCC(CC1)C2=CC(=CC(=C2)CCC)CCC)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL372274 mshr_human Human No 6.7 EC50 = 210 Funct
Effective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cellsEffective concentration required for cAMP accumulation mediated by human Melanocortin 1 receptor in HEK293 cells
933 26 9 7 6.0 CCCCC(=O)NC1(CCC(CC1)C2=CC(=CC(=C2)CCC)CCC)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL204078 mshr_human Human No 5.7 EC50 = 2100 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
621 8 2 5 6.3 CC1COC(=O)N1CC2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)C6CCCCC6
CHEMBL204078 mshr_human Human No 5.7 EC50 = 2100 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
621 8 2 5 6.3 CC1COC(=O)N1CC2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)C6CCCCC6
CHEMBL3577990 mshr_mouse Mouse No 4.7 EC50 = 21000 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
963 11 9 10 0.3 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)C4=CC=CC=C4)CC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL3577990 mshr_mouse Mouse No 4.7 EC50 = 21000 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
963 11 9 10 0.3 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)C4=CC=CC=C4)CC5=CC=CC=C5)CCCN=C(N)N)CC6=CC=CC=C6
CHEMBL185869 mshr_human Human No 6.7 EC50 = 211 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
760 20 8 7 2.9 CCOC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL185869 mshr_human Human No 6.7 EC50 = 211 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
760 20 8 7 2.9 CCOC(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3600915 mshr_human Human No 6.7 EC50 = 214 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL3600915 mshr_human Human No 6.7 EC50 = 214 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL364359 mshr_human Human No 5.7 EC50 = 2157 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
820 19 8 11 3.5 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NS(=O)(=O)C(F)(F)F
CHEMBL364359 mshr_human Human No 5.7 EC50 = 2157 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
820 19 8 11 3.5 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NS(=O)(=O)C(F)(F)F
CHEMBL410435 mshr_mouse Mouse No 4.7 EC50 = 21600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
500 6 1 2 5.9 CC1=CC=CC2=C1N(C(=O)C(NC2=O)CC3=CN(C4=CC=CC=C43)CC5=CC=CC=C5)CC6=CC=CC=C6
CHEMBL410435 mshr_mouse Mouse No 4.7 EC50 = 21600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
500 6 1 2 5.9 CC1=CC=CC2=C1N(C(=O)C(NC2=O)CC3=CN(C4=CC=CC=C43)CC5=CC=CC=C5)CC6=CC=CC=C6
CHEMBL361252 mshr_human Human No 5.7 EC50 = 2162 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
759 18 8 6 2.2 CN(C)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL361252 mshr_human Human No 5.7 EC50 = 2162 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
759 18 8 6 2.2 CN(C)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL212332 mshr_human Human No 4.7 EC50 = 21667 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
550 13 6 6 1.9 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=C(C=C3)F)N
CHEMBL212332 mshr_human Human No 4.7 EC50 = 21667 Funct
Agonist activity at human MC1RAgonist activity at human MC1R
550 13 6 6 1.9 CNC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CC=C(C=C3)F)N
CHEMBL3600912 mshr_human Human No 7.7 EC50 = 22 Funct
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3287328 mshr_mouse Mouse No 7.7 EC50 = 22 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
748 15 6 8 1.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(CC4=CC=C(C=C4)[N+](=O)[O-])C(=O)N
CHEMBL3646892 mshr_human Human No 7.7 EC50 = 22 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1055 18 14 12 -2.8 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCCCNC(=O)CC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CC4=CC=CC=C4C=C3)C(=O)N
CHEMBL3600912 mshr_human Human No 7.7 EC50 = 22 Funct
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1102 17 11 11 1.6 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3287328 mshr_mouse Mouse No 7.7 EC50 = 22 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
748 15 6 8 1.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)N2CC3=CC=CC=C3CC2C(=O)NC(CC4=CC=C(C=C4)[N+](=O)[O-])C(=O)N
CHEMBL405791 mshr_mouse Mouse No 7.7 EC50 = 22 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1146 18 14 14 0.7 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC5=CC=CC=C54)CC6=NC=CN6)NC(=O)C(CC7=CC=CC=C7)N)O
CHEMBL2369971 mshr_mouse Mouse No 7.7 EC50 = 22.1 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1447 21 17 18 -2.2 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)N2CCCC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)CC5=CC=CC=C5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL2369971 mshr_mouse Mouse No 7.7 EC50 = 22.1 Funct
Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor
1447 21 17 18 -2.2 CC1C(=O)NC(C(=O)NC(N(C(=O)CC(C(=O)N2CCCC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)CC5=CC=CC=C5)NC(=O)C(CC6=CC=C(C=C6)O)N)C(CC7=CC=C(C=C7)O)C(=O)N)(C)C(=O)O)CC8=CC=CC=C8
CHEMBL591037 mshr_human Human No 7.7 EC50 = 22.4 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
592 8 1 8 5.4 CC(C)N(C1=CC=C(C=C1)OC(F)(F)F)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL591037 mshr_human Human No 7.7 EC50 = 22.4 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
592 8 1 8 5.4 CC(C)N(C1=CC=C(C=C1)OC(F)(F)F)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL589468 mshr_mouse Mouse No 6.7 EC50 = 220 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
850 12 8 8 0.4 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)C(NC(=O)CN(C(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL602651 mshr_mouse Mouse No 6.7 EC50 = 220 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 9 8 -0.1 CC(=O)NCC(=O)NC(CC1=CC=CC=C1)C(=O)N(CC2=CC=CC=C2)CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL2113043 mshr_human Human No 6.7 EC50 = 220 Funct
Effective concentration against human melanocortin 1 receptor in cAMP release assayEffective concentration against human melanocortin 1 receptor in cAMP release assay
623 10 2 7 5.8 CC(CCC1CC(=NN(C1=O)C2=CC=C(C=C2)OC)SC3=CC=C(C=C3)Cl)NC(=O)C4CCNCC4C5=CC=C(C=C5)F
CHEMBL589468 mshr_mouse Mouse No 6.7 EC50 = 220 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
850 12 8 8 0.4 C1CC(=O)NCCN(C(=O)C(NC(=O)C(NC(=O)C(NC(=O)CN(C(=O)C1)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)CC(=O)N
CHEMBL602651 mshr_mouse Mouse No 6.7 EC50 = 220 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 9 8 -0.1 CC(=O)NCC(=O)NC(CC1=CC=CC=C1)C(=O)N(CC2=CC=CC=C2)CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL2113043 mshr_human Human No 6.7 EC50 = 220 Funct
Effective concentration against human melanocortin 1 receptor in cAMP release assayEffective concentration against human melanocortin 1 receptor in cAMP release assay
623 10 2 7 5.8 CC(CCC1CC(=NN(C1=O)C2=CC=C(C=C2)OC)SC3=CC=C(C=C3)Cl)NC(=O)C4CCNCC4C5=CC=C(C=C5)F
CHEMBL429212 mshr_human Human No 6.7 EC50 = 220 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
603 7 2 7 3.4 COC1=CC=C(C=C1)CC(C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)NC(=O)C5CC6=CC=CC=C6CN5
CHEMBL104397 mshr_mouse Mouse No 4.7 EC50 = 22000 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
736 18 9 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL3600834 mshr_human Human No 5.7 EC50 = 2210 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1088 17 12 11 1.5 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600834 mshr_human Human No 5.7 EC50 = 2210 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1088 17 12 11 1.5 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL303283 mshr_mouse Mouse No 4.7 EC50 = 22300 Funct
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cellsAgonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
436 12 5 3 2.6 C1=CC=C(C=C1)CNC(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NCCCCCCN
CHEMBL433522 mshr_mouse Mouse No 5.7 EC50 = 2240 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
648 18 8 8 -1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=NC=C3)C(=O)N
CHEMBL3421677 mshr_human Human No 6.7 EC50 = 226 Funct
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
765 15 8 7 1.8 CC(=O)NC1CC2=C(CN(C1=O)C(CC3=CC=C(C=C3)F)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N)NC6=CC=CC=C26
CHEMBL3421677 mshr_human Human No 6.7 EC50 = 226 Funct
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterActivity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
765 15 8 7 1.8 CC(=O)NC1CC2=C(CN(C1=O)C(CC3=CC=C(C=C3)F)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N)NC6=CC=CC=C26
CHEMBL1093305 mshr_human Human No 6.6 EC50 = 228 Funct
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
600 5 1 5 5.8 CC1=C(C=C2C(=C1)C(CC23CCN(CC3)C(=O)C4CN(CC4C5=C(C=C(C=C5)F)F)C(C)(C)C)C(C)(C)NC(=O)C)Cl
CHEMBL1093305 mshr_human Human No 6.6 EC50 = 228 Funct
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
600 5 1 5 5.8 CC1=C(C=C2C(=C1)C(CC23CCN(CC3)C(=O)C4CN(CC4C5=C(C=C(C=C5)F)F)C(C)(C)C)C(C)(C)NC(=O)C)Cl
CHEMBL264190 mshr_human Human Yes 6.6 EC50 = 228 Funct
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL104052 mshr_mouse Mouse No 4.6 EC50 = 22900 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
687 18 9 8 -1.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CN=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3600918 mshr_human Human No 7.6 EC50 = 23 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL365019 mshr_human Human No 7.6 EC50 = 23 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
862 23 8 7 4.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CCCC(=O)C5=CC=CC=C5
CHEMBL3600918 mshr_human Human No 7.6 EC50 = 23 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL365019 mshr_human Human No 7.6 EC50 = 23 Funct
Agonistic activity against human Melanocortin 1 receptorAgonistic activity against human Melanocortin 1 receptor
862 23 8 7 4.1 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)CCCC(=O)C5=CC=CC=C5
CHEMBL406614 mshr_human Human No 7.6 EC50 = 23 Funct
Agonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assayAgonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assay
1145 19 14 12 1.1 CC(C)C(C(=O)NC(C(C)C)C(=O)NCC(=O)N)NC(=O)C1CCC(=O)NCCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC5=CC=CC=C5C=C4)CC6=CN=CN6
CHEMBL2371590 mshr_human Human No 7.6 EC50 = 23 Funct
Agonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assayAgonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assay
1123 22 14 12 1.4 CCCCC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CCC(=O)N1)C(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NCC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL273044 mshr_mouse Mouse No 6.6 EC50 = 230 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
433 5 1 2 5.5 C1=CC=C(C=C1)CC2C(=O)N(C3=CC=CC=C3C(=O)N2)CC4=CC=CC=C4C5=CC=CC=C5
CHEMBL29056 mshr_human Human No 6.6 EC50 = 230 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
705 20 9 7 0.1 CCCC(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NCC(=O)N
CHEMBL273044 mshr_mouse Mouse No 6.6 EC50 = 230 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
433 5 1 2 5.5 C1=CC=C(C=C1)CC2C(=O)N(C3=CC=CC=C3C(=O)N2)CC4=CC=CC=C4C5=CC=CC=C5
CHEMBL517108 mshr_human Human No 5.6 EC50 = 2300 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
491 7 2 5 3.2 CC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL500516 mshr_mouse Mouse No 5.6 EC50 = 2300 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
701 18 10 8 -0.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL152555 mshr_mouse Mouse No 5.6 EC50 = 2300 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
723 19 8 7 1.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(C(C3=CC=CC=C3)C4=CC=CC=C4)C(=O)N
CHEMBL517108 mshr_human Human No 5.6 EC50 = 2300 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC1R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
491 7 2 5 3.2 CC1C(=O)N(CCN1C(=O)C(CC2=CC=C(C=C2)F)N)C(CC3=CC4=CC=CC=C4C=C3)C(=O)NC
CHEMBL500516 mshr_mouse Mouse No 5.6 EC50 = 2300 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
701 18 10 8 -0.7 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL212766 mshr_human Human No 6.6 EC50 = 232 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
516 11 3 4 3.1 CC(=O)NC(CC1=CC=CC=C1)C(=O)N2CC(CC2CCCN=C(N)N)OCC3=CC4=CC=CC=C4C=C3
CHEMBL212766 mshr_human Human No 6.6 EC50 = 232 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
516 11 3 4 3.1 CC(=O)NC(CC1=CC=CC=C1)C(=O)N2CC(CC2CCCN=C(N)N)OCC3=CC4=CC=CC=C4C=C3
CHEMBL102688 mshr_mouse Mouse No 5.6 EC50 = 2350 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
712 16 9 7 0.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC2(CCC3=CC=CC=C3C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL50056 mshr_mouse Mouse Yes 5.6 EC50 = 2360 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL50056 mshr_mouse Mouse Yes 5.6 EC50 = 2360 Funct
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL209587 mshr_human Human No 7.6 EC50 = 24 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
640 14 6 7 0.9 C1C(CN(C1C(=O)NCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C(CC3=CN=CN3)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL3287329 mshr_mouse Mouse No 7.6 EC50 = 24 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
826 20 9 7 0.2 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)N
CHEMBL209587 mshr_human Human No 7.6 EC50 = 24 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
640 14 6 7 0.9 C1C(CN(C1C(=O)NCCN=C(N)N)C(=O)C(CC2=CC=CC=C2)NC(=O)C(CC3=CN=CN3)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL3287329 mshr_mouse Mouse No 7.6 EC50 = 24 Funct
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
826 20 9 7 0.2 CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC1=CC=C(C=C1)Cl)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CC=C(C=C2)I)C(=O)N
CHEMBL3799563 mshr_mouse Mouse No 7.6 EC50 = 24.9 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
962 35 11 13 -1.4 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)COCC(=O)NCCCOCCOCCOCCCN
CHEMBL3799563 mshr_mouse Mouse No 7.6 EC50 = 24.9 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
962 35 11 13 -1.4 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)N)NC(=O)C(CC4=CN=CN4)NC(=O)COCC(=O)NCCCOCCOCCOCCCN
CHEMBL271586 mshr_mouse Mouse No 6.6 EC50 = 240 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
878 12 9 8 1.4 C1CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(CCCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL589308 mshr_mouse Mouse No 6.6 EC50 = 240 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 8 8 -0.1 CC(=O)NCC(=O)N(CC1=CC=CC=C1)CC(=O)N(CC2=CC=CC=C2)CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL1688106 mshr_mouse Mouse Yes 6.6 EC50 = 240 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CC=CC=C3)C(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CNC=N6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL2113039 mshr_human Human No 6.6 EC50 = 240 Funct
Effective concentration against human melanocortin 1 receptor in cAMP release assayEffective concentration against human melanocortin 1 receptor in cAMP release assay
609 10 2 7 5.4 CC(CCC1CC(=NN(C1=O)C2=CC=C(C=C2)OC)SC3=CC=C(C=C3)Cl)NC(=O)C4CNCC4C5=CC=C(C=C5)F
CHEMBL271586 mshr_mouse Mouse No 6.6 EC50 = 240 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
878 12 9 8 1.4 C1CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(CCCNC(=O)C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL589308 mshr_mouse Mouse No 6.6 EC50 = 240 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase reporter gene assay
810 22 8 8 -0.1 CC(=O)NCC(=O)N(CC1=CC=CC=C1)CC(=O)N(CC2=CC=CC=C2)CC(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL1688106 mshr_mouse Mouse Yes 6.6 EC50 = 240 Funct
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
1636 24 20 21 0.6 CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC2CSCC(=O)N(CC(NC2=O)CC3=CC=CC=C3)C(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CNC5=CC=CC=C54)CCCNC(=N)N)CC6=CNC=N6)NC(=O)C(CC7=CC=C(C=C7)O)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)CC9=CC=CC=C9
CHEMBL2113039 mshr_human Human No 6.6 EC50 = 240 Funct
Effective concentration against human melanocortin 1 receptor in cAMP release assayEffective concentration against human melanocortin 1 receptor in cAMP release assay
609 10 2 7 5.4 CC(CCC1CC(=NN(C1=O)C2=CC=C(C=C2)OC)SC3=CC=C(C=C3)Cl)NC(=O)C4CNCC4C5=CC=C(C=C5)F
CHEMBL3646884 mshr_human Human No 7.6 EC50 = 25 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1044 18 15 12 -3.9 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCCNC(=O)CCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL264190 mshr_mouse Mouse Yes 7.6 EC50 = 25.6 Funct
Functional activity at the mouse melanocortin 1 receptorFunctional activity at the mouse melanocortin 1 receptor
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3601432 mshr_human Human No 7.6 EC50 = 25.7 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1144 17 8 11 2.2 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL3601432 mshr_human Human No 7.6 EC50 = 25.7 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1144 17 8 11 2.2 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL1761874 mshr_human Human No 6.6 EC50 = 250 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
572 7 3 5 4.7 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL1761874 mshr_human Human No 6.6 EC50 = 250 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
572 7 3 5 4.7 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL3576882 mshr_mouse Mouse No 5.6 EC50 = 2500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
999 10 9 10 1.4 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC4=CC5=CC=CC=C5C=C4C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3577986 mshr_mouse Mouse No 5.6 EC50 = 2500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CC5=CC=CC6=CC=CC=C65)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL154251 mshr_mouse Mouse No 5.6 EC50 = 2500 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
647 18 8 7 -0.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=CC=C3)C(=O)N
CHEMBL3576882 mshr_mouse Mouse No 5.6 EC50 = 2500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
999 10 9 10 1.4 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC4=CC5=CC=CC=C5C=C4C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC6=CC=CC=C6)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL3577986 mshr_mouse Mouse No 5.6 EC50 = 2500 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassayAgonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay
1027 12 9 10 1.9 CC1C(=O)NC(C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC4=CC=CC=C4)CC5=CC=CC6=CC=CC=C65)CCCN=C(N)N)CC7=CC=CC=C7
CHEMBL322889 mshr_mouse Mouse No 4.6 EC50 = 25100 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
725 18 10 7 0.1 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL309869 mshr_human Human No 6.6 EC50 = 255 Funct
Agonist potency for human Melanocortin 1 receptorAgonist potency for human Melanocortin 1 receptor
771 25 9 8 3.1 CCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCCNC(C)C)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL3601428 mshr_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL1775066 mshr_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulationAgonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation
992 15 13 10 -0.4 CC1C(=O)NC(C(=O)NC(CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)C(=O)N)CC5=CC=CC=C5
CHEMBL3646889 mshr_human Human No 7.6 EC50 = 26 Funct
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
1058 19 15 12 -3.5 CC(=O)NC(CCCN=C(N)N)C(=O)NC1CCNC(=O)CCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCC(=O)N)CC2=CC=CC=C2)CCCN=C(N)N)CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3601428 mshr_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC(=O)C(N(C1=O)C)CC2=CN=CN2)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL1775066 mshr_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulationAgonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation
992 15 13 10 -0.4 CC1C(=O)NC(C(=O)NC(CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)C(=O)N)CC5=CC=CC=C5
CHEMBL3753760 mshr_human Human No 7.6 EC50 = 26 Funct
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
1170 17 13 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC1=O)CC3=CNC4=CC=CC=C43)CC5=CC=CC=C5)CCCN=C(N)N)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL3797690 mshr_mouse Mouse No 7.6 EC50 = 26.2 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1004 36 11 13 -1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N
CHEMBL3797690 mshr_mouse Mouse No 7.6 EC50 = 26.2 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
1004 36 11 13 -1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N
CHEMBL1761873 mshr_human Human No 6.6 EC50 = 260 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
572 7 3 5 4.7 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL1761873 mshr_human Human No 6.6 EC50 = 260 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
572 7 3 5 4.7 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)F)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL204308 mshr_human Human No 5.6 EC50 = 2600 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
633 8 2 5 6.2 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C(=O)OCC67CC7
CHEMBL105113 mshr_mouse Mouse No 5.6 EC50 = 2600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
702 18 10 8 -0.4 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL204308 mshr_human Human No 5.6 EC50 = 2600 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
633 8 2 5 6.2 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C(=O)OCC67CC7
CHEMBL105113 mshr_mouse Mouse No 5.6 EC50 = 2600 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
702 18 10 8 -0.4 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL96871 mshr_mouse Mouse No 5.6 EC50 = 2600 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
708 15 7 6 1.6 CC(=O)N1CC2=CC=CC=C2CC1C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL379531 mshr_human Human Yes 6.6 EC50 = 269.9 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
712 10 9 7 0.5 C1CC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL379531 mshr_human Human Yes 6.6 EC50 = 269.9 Funct
Activity at human MC1R by cAMP accumulation in SaoS2 cellsActivity at human MC1R by cAMP accumulation in SaoS2 cells
712 10 9 7 0.5 C1CC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL524861 mshr_human Human No 5.6 EC50 = 2700 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1041 16 13 11 -1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CC(CN2C1=O)N=C(N)N)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3422430 mshr_mouse Mouse No 5.6 EC50 = 2700 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
834 15 7 6 2.2 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)N4CC5=CC=CC=C5CC4C(=O)N
CHEMBL524861 mshr_human Human No 5.6 EC50 = 2700 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
1041 16 13 11 -1.3 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CC(CN2C1=O)N=C(N)N)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL3422430 mshr_mouse Mouse No 5.6 EC50 = 2700 Funct
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
834 15 7 6 2.2 CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=C(C=C3)I)C(=O)NC(CCCN=C(N)N)C(=O)N4CC5=CC=CC=C5CC4C(=O)N
CHEMBL263607 mshr_human Human No 5.6 EC50 = 2700 Funct
Agonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assayAgonistic activity towards Melanocortin 1 receptor in the Xenopus frog skin assay
1095 19 14 12 -0.2 CC(C)C(C(=O)NC(C(C)C)C(=O)NCC(=O)N)NC(=O)C1CCC(=O)NCCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5
CHEMBL140324 mshr_mouse Mouse No 4.6 EC50 = 27000 Funct
Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells
686 20 4 7 0.7 CC(=O)N(CCC1=CN=CN1)CC(=O)N(CC2=CC=CC=C2)CC(=O)N(CCCCN)CC(=O)N(CCC3=CNC4=CC=CC=C43)CC(=O)N
CHEMBL3601430 mshr_human Human No 6.6 EC50 = 273 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL3601430 mshr_human Human No 6.6 EC50 = 273 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1130 17 9 11 2.0 CCCCC(C(=O)NC1CC(=O)NCCCCC(N(C(=O)C(NC(=O)C(N(C(=O)C(N(C(=O)C(N(C1=O)C)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C)C(=O)N)NC(=O)C
CHEMBL567240 mshr_mouse Mouse No 6.6 EC50 = 274 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
604 16 8 7 0.3 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC(=CC=C3)O
CHEMBL567240 mshr_mouse Mouse No 6.6 EC50 = 274 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
604 16 8 7 0.3 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C=CC3=CC(=CC=C3)O
CHEMBL346930 mshr_human Human No 6.6 EC50 = 274 Funct
Effective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulationEffective concentration against hMC1R using HEK293 cells was determined by measuring the cAMP accumulation
788 22 9 9 1.1 CCCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CSC4=CC=CC=C43)C(=O)NCC(=O)N
CHEMBL3600920 mshr_human Human No 6.6 EC50 = 276 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL3600920 mshr_human Human No 6.6 EC50 = 276 Funct
Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
1116 17 10 11 1.8 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(N(C(=O)C(N(C(=O)C(N(C(=O)C(NC1=O)CC2=CN=CN2)C)CC3=CC4=CC=CC=C4C=C3)C)CCCN=C(N)N)C)CC5=CNC6=CC=CC=C65)C(=O)N)NC(=O)C
CHEMBL349795 mshr_mouse Mouse No 5.6 EC50 = 2780 Funct
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
653 18 8 8 -0.4 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CC=CS3)C(=O)N
CHEMBL569220 mshr_mouse Mouse No 5.6 EC50 = 2790 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 16 7 7 0.9 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C(=CC3=CC=CC=C3)F
CHEMBL569220 mshr_mouse Mouse No 5.6 EC50 = 2790 Funct
Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R
606 16 7 7 0.9 C1=CC=C(C=C1)CC(C(=O)NC(CCCN=C(N)N)C(=O)N)NC(=O)C(CC2=CN=CN2)NC(=O)C(=CC3=CC=CC=C3)F
CHEMBL210011 mshr_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
585 12 4 5 3.6 C1CCNC(C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL2371966 mshr_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
1015 12 8 9 4.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCCN2C(=O)C(NC(=O)C3CCCN3C1=O)CC4=CC=C(C=C4)C5=CC=CC=C5)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL272660 mshr_mouse Mouse No 7.6 EC50 = 28 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
850 12 9 8 0.7 C1CNC(=O)CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL210011 mshr_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
585 12 4 5 3.6 C1CCNC(C1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3CCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL2371966 mshr_human Human No 7.6 EC50 = 28 Funct
Agonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulationAgonist activity at human melanocortin receptor 1b expressed in CHO cells assessed as cAMP accumulation
1015 12 8 9 4.1 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C2CCCCN2C(=O)C(NC(=O)C3CCCN3C1=O)CC4=CC=C(C=C4)C5=CC=CC=C5)CC6=CNC7=CC=CC=C76)C(=O)N)NC(=O)C
CHEMBL272660 mshr_mouse Mouse No 7.6 EC50 = 28 Funct
Agonist activity at mouse MC1R expressed in HEK293 cellsAgonist activity at mouse MC1R expressed in HEK293 cells
850 12 9 8 0.7 C1CNC(=O)CCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N(C1)CC(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CC=CC=C5
CHEMBL14642 mshr_human Human Yes 7.6 EC50 = 28 Funct
In vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 1 receptor (MC1R) in SPA-based cAMP assay in melanoma cells
560 12 2 6 2.7 CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)C(CC3=CN=CN3C)N)C4=CC=CC=C4
CHEMBL319871 mshr_mouse Mouse No 7.6 EC50 = 28.4 Funct
Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)
762 19 9 7 1.6 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)N
CHEMBL2364550 mshr_human Human No 7.5 EC50 = 28.6 Funct
Decrease in frog skin reflectivity (metabotropic activity).Decrease in frog skin reflectivity (metabotropic activity).
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL2364550 mshr_human Human No 7.5 EC50 = 28.6 Funct
Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL1762009 mshr_human Human No 6.6 EC50 = 280 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
588 7 3 4 5.2 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL448536 mshr_mouse Mouse No 6.6 EC50 = 280 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
711 18 9 8 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C#N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL1762009 mshr_human Human No 6.6 EC50 = 280 Funct
Agonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC1 receptor expressed in CHO cells assessed as cAMP accumulation
588 7 3 4 5.2 CC1CN(CC(N1)C)C(=O)NC(CC2=CC=C(C=C2)Cl)C(=O)N3CCC(CC3)(C4CCCCC4)C(=O)NC(C)(C)C
CHEMBL448536 mshr_mouse Mouse No 6.6 EC50 = 280 Funct
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
711 18 9 8 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)C#N)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL61681 mshr_mouse Mouse No 4.6 EC50 = 28000 Funct
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cellsAgonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
441 8 4 2 4.0 CC1=CC(=CC=C1)CNC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)NCC4=CC=CC=C4
CHEMBL2370696 mshr_mouse Mouse No 4.6 EC50 = 28100 Funct
Agonist activity against mouse melanocortin-1 receptorAgonist activity against mouse melanocortin-1 receptor
1323 21 17 16 -0.5 CC1C(=O)NC(C(=O)NC(CC(=O)NCCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CCCN=C(N)N)NC(=O)C(CC4=CC=C(C=C4)O)N)C(=O)NC(CC5=CC=C(C=C5)O)C(=O)N)CC6=CC=CC=C6
CHEMBL339053 mshr_human Human Yes 5.5 EC50 = 2850 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
589 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C=NC=N6
CHEMBL339053 mshr_human Human Yes 5.6 EC50 = 2850 Funct
Activity against human MC1BR by cAMP accumulationActivity against human MC1BR by cAMP accumulation
589 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C=NC=N6
CHEMBL339053 mshr_human Human Yes 5.6 EC50 = 2850 Funct
Functional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC1R) receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human melanocortin 1 (MC1R) receptor
589 8 2 5 5.9 C1CCC(CC1)C2(CCN(CC2)C(=O)C(CC3=CC=C(C=C3)Cl)NC(=O)C4CC5=CC=CC=C5CN4)CN6C=NC=N6
CHEMBL94391 mshr_mouse Mouse No 6.5 EC50 = 289 Funct
In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor.
686 18 9 7 -0.3 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL598631 mshr_human Human No 7.5 EC50 = 29.5 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL598631 mshr_human Human No 7.5 EC50 = 29.5 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
538 8 1 5 4.2 CC(C)N(C1=CC=C(C=C1)OC)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL371215 mshr_human Human No 5.5 EC50 = 2900 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
911 21 8 7 4.6 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2Br)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NCC(=O)N
CHEMBL371215 mshr_human Human No 5.5 EC50 = 2900 Funct
Agonist activity in HEK293 cells transfected with human MC1R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC1R by cAMP accumulation
911 21 8 7 4.6 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2Br)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NCC(=O)N
CHEMBL442339 mshr_human Human No 5.5 EC50 = 2910 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
900 21 9 7 3.4 CCCCC(=O)NC1(CCC2=C(C1)C(=CC=C2)Br)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL434966 mshr_human Human No 6.5 EC50 = 295 Funct
Agonist activity against human melanocortin receptor hMC1RAgonist activity against human melanocortin receptor hMC1R
863 22 9 7 3.9 CCCCC(=O)NC1(CCC2=C(C1)C=CC=C2C(C)C)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NCC(=O)N
CHEMBL598643 mshr_human Human No 6.5 EC50 = 295.1 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
508 7 1 4 4.2 CC(C)N(C1=CC=CC=C1)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL598643 mshr_human Human No 6.5 EC50 = 295.1 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
508 7 1 4 4.2 CC(C)N(C1=CC=CC=C1)C(=O)CN2C=CN(C(=O)C(C2=O)CC3=C4C=CC=CC4=NN3)C5=CC=CC=C5
CHEMBL590841 mshr_human Human No 5.5 EC50 = 2951.2 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
556 8 1 6 4.1 CC(C)N(C1=CC=C(C=C1)F)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)C5=CC=CC=C5
CHEMBL590841 mshr_human Human No 5.5 EC50 = 2951.2 Funct
Agonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC1R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
556 8 1 6 4.1 CC(C)N(C1=CC=C(C=C1)F)C(=O)CN2C=CN(C(=O)C(C2=O)(CC3=C4C=CC=CC4=NN3)OC)C5=CC=CC=C5
CHEMBL2370964 mshr_human Human Yes 8.5 EC50 = 3 Funct
Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 minsAgonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins
1602 49 23 19 -0.2 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)N
CHEMBL378293 mshr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
682 15 6 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL2371903 mshr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
961 13 10 9 1.5 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2C3=CC=CC=C3CN2C1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL378293 mshr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human MC1R transfected in HEK293 cellsAgonist activity at human MC1R transfected in HEK293 cells
682 15 6 7 1.2 CC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)N3CC(CC3C(=O)NCCN=C(N)N)OCC4=CC5=CC=CC=C5C=C4
CHEMBL2371903 mshr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human melanocortin receptor (hMC1R).Agonist activity at human melanocortin receptor (hMC1R).
961 13 10 9 1.5 CCCCC(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2C3=CC=CC=C3CN2C1=O)CC4=CC=CC=C4)CCCN=C(N)N)CC5=CNC6=CC=CC=C65)C(=O)N
CHEMBL2364550 mshr_human Human No 8.5 EC50 = 3 Funct
Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generationEffective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation
1038 17 13 11 0.4 CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)C(C)C4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
CHEMBL413439 mshr_human Human No 8.5 EC50 = 3 Funct
Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)
1603 47 21 20 -0.3 CCCCC(C(=O)NCC(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC4=CNC5=CC=CC=C54)C(=O)NC(CC(=O)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NCC(=O)O)NC(=O)C(C(C)C)NC(=O)C(CC7=CC=C(C=C7)O)N
CHEMBL407845 mshr_mouse Mouse No 8.5 EC50 = 3 Funct
Maximal agonist response of mouse melanocortin 1 receptor (MC1R)Maximal agonist response of mouse melanocortin 1 receptor (MC1R)
1096 18 14 14 -0.6 CC(C(C(=O)N)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5)NC(=O)C(CC6=CC=CC=C6)N)O
CHEMBL195468 mshr_mouse Mouse No 8.5 EC50 = 3.1 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
812 29 9 7 5.8 CCCCCCCCCCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL195468 mshr_mouse Mouse No 8.5 EC50 = 3.1 Funct
In vitro agonist potency for Mouse Melanocortin 1 receptorIn vitro agonist potency for Mouse Melanocortin 1 receptor
812 29 9 7 5.8 CCCCCCCCCCCCNC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)N
CHEMBL3600736 mshr_human Human No 8.5 EC50 = 3.3 Funct
Agonist activity at